b Alia-Ranbir's Daughter Raha Turns 2 By www.rediff.com Published On :: Alia Bhatt and Ranbir Kapoor's little girl Raha turned two on November 6, and we were treated to the most adorable pictures on social media. Full Article
b Why Abhishek Missed Aishwarya's Birthday By www.rediff.com Published On :: When Aishwarya celebrated her birthday in Dubai on November 1, the speculation regarding the Abhishek-Aishwarya marital rift ran even higher. Full Article
b Design, synthesis, inhibitory activity, and molecular simulations study for D-glucose-conjugated thioureas containing pyrimidine ring as multitarget inhibitors against α-amylase, α-glucosidase, DDP-4, and PTP1B in Type 2 diabetes mellitus By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3395-3417DOI: 10.1039/D4MD00334A, Research ArticleVu Ngoc Toan, Do Son Hai, Hoang Thi Kim Van, Nguyen Minh Tri, Duong Ngoc Toan, Nguyen Thi Thanh Mai, Nguyen Dinh ThanhD-Glucose-conjugated thioureas from 2-aminopyrimidines had inhibitory activity against α-amylase, α-glucosidase, DPP-4, PTP1B. The cytotoxicity, inhibitory kinetics, and molecular simulations of the most potent inhibitors 8k, 8j, 8f, and 8h were studied.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Lead optimisation of OXS007417: in vivo PK profile and hERG liability modulation to optimise a small molecule differentiation agent for the potential treatment of acute myeloid leukaemia By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3495-3506DOI: 10.1039/D4MD00275J, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Thomas J. Cogswell, Laia Josa-Culleré, David Zimmer, Sébastien R. G. Galan, Morgan Jay-Smith, Kate S. Harris, Carole J. R. Bataille, Thomas R. Jackson, Douzi Zhang, Stephen G. Davies, Paresh Vyas, Thomas A. Milne, Graham M. Wynne, Angela J. RussellThe optimisation of a class of AML differentiation agents is described to show improved potency, solubility and stability, reduced off target toxicity, and tumour regression in a murine model in vivo.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Integrating amino acids into Bcr-Abl inhibitors: design, synthesis, biological evaluation, and in silico studies By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3507-3528DOI: 10.1039/D4MD00417E, Research ArticleYuying Liu, Zeyu Yang, Jie Zhang, Na Guo, Nanxin Liu, Qingqing Zhang, Xintao Dang, Yanchen Li, Jie Zhang, Xiaoyan PanIn continuation of our previous research, a series of novel Bcr-AblT315I inhibitors with tert-leucine or serine as a flexible linker were developed and biological evaluation was performed in vitro.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3576-3596DOI: 10.1039/D4MD00438H, Research ArticleRuolin Cao, Fangyu Du, Zhiqiang Liu, Pengcheng Cai, Minggang Qi, Wei Xiao, Xuefei Bao, Guoliang ChenRho-associated coiled-coil containing kinase (ROCK) plays an important role in inflammation.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Discovery of highly potent SARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3469-3476DOI: 10.1039/D4MD00422A, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Hugo Kocek, Dominika Chalupská, Milan Dejmek, Alexandra Dvořáková, Michala Zgarbová, Michal Šála, Karel Chalupský, Petra Krafčíková, Tomáš Otava, Matúš Drexler, Eliška Procházková, Blanka Klepetářová, Milan Štefek, Ján Kozic, Helena Mertlíková-Kaiserová, Evzen Boura, Jan Weber, Radim NenckaSARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Synthesis and cytotoxic activity of madecassic acid–silybin conjugate compounds in liver cancer cells By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3418-3432DOI: 10.1039/D4MD00170B, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Chien Van Tran, Thao Thi Phuong Tran, Anh The Nguyen, Loc Van Tran, Ninh Thi Pham, Luu Thi Nguyen, Dung Thi Nguyen, Michelle D. Garrett, Nga Thi Nguyen, Thao Thi Do, Christopher J. Serpell, Sung Van TranMadecassic acid and silybin have been conjoined to produce hybrid compounds with improved and different activity against liver cancer cells.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Synthesis of a celastrol derivative as a cancer stem cell inhibitor through regulation of the STAT3 pathway for treatment of ovarian cancer By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3433-3443DOI: 10.1039/D4MD00468J, Research ArticleMeijuan Liu, Na Li, Zhaoxue Wang, Shuo Wang, Shaoda Ren, Xiaojing LiA synthetic celastrol derivative (Cel-N) attenuates cancer cell stemness, inhibits the STAT3 pathway, and exerts anti-ovarian cancer effects in cell and mouse models.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3529-3557DOI: 10.1039/D4MD00481G, Research ArticleMohamed K. S. El-Nagar, Mai I. Shahin, Mohammed F. El-Behairy, Ehab S. Taher, Mohamed F. El-Badawy, Marwa Sharaky, Dalal A. Abou El Ella, Khaled A. M. Abouzid, Mai AdelDiscovery of novel pyridazinone derivatives with dual antimicrobial and anticancer activities.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Design, synthesis and biological evaluation of a novel PSMA–PI3K small molecule drug conjugate By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3485-3494DOI: 10.1039/D4MD00246F, Research ArticleShouguo Peng, Haixia Li, Weilu Cui, Tianning Xiong, Jiaqi Hu, Haixiang Qi, Songwen Lin, Deyu Wu, Ming Ji, Heng XuA novel PSMA–PI3K small molecule drug conjugate has been prepared, highlighting its potential in targeted cancer therapy.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3477-3484DOI: 10.1039/D4MD00266K, Research ArticleRaitis Bobrovs, Svetlana Terentjeva, Ninni Elise Olafsen, Zilvinas Dambrauskas, Antanas Gulbinas, Toivo Maimets, Indrek Teino, Aigars Jirgensons, Jason Matthews, Kristaps JaudzemsThe aryl hydrocarbon receptor (AHR) is a versatile ligand-dependent transcription factor involved in diverse biological processes, from metabolic adaptations to immune system regulation.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019–2024) By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3371-3394DOI: 10.1039/D4MD00384E, Review ArticleDebasis Das, Lingzhi Xie, Jian HongProspects of novel fourth-generation EGFR-TKIs overcoming C797S-mediated resistance in non-small cell lung cancer.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Rationally modified SNX-class Hsp90 inhibitors disrupt extracellular fibronectin assembly without intracellular Hsp90 activity By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3609-3615DOI: 10.1039/D4MD00501E, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Gciniwe S. Mathenjwa, Abir Chakraborty, Abantika Chakraborty, Ronel Muller, Mathew P. Akerman, Moira L. Bode, Adrienne L. Edkins, Clinton G. L. VealeRationally modified Hsp90 inhibitors which retained of on-target activity but showed no engagement of intracellular Hsp90, or stimulation of the heat shock response, were found to significantly alter the extracellular fibronectin network.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Exploring apoptotic induction of malabaricone A in triple-negative breast cancer cells: an acylphenol phyto-entity isolated from the fruit rind of Myristica malabarica Lam. By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3558-3575DOI: 10.1039/D4MD00391H, Research ArticlePothiyil S. Vimalkumar, Neethu Sivadas, Vishnu Priya Murali, Daisy R. Sherin, Madhukrishnan Murali, Anuja Gracy Joseph, Kokkuvayil Vasu Radhakrishnan, Kaustabh Kumar MaitiMalabaricone A isolated from Myristica malabarica induces apoptosis in triple-negative breast cancer cells through intrinsic and extrinsic pathways, which is validated through in vitro and in silico studies and resembles a potent phyto-entity.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3597-3608DOI: 10.1039/D4MD00378K, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Rachel A. Heylen, Nicola Cusick, Tom White, Emily J. Owen, Bethany L. Patenall, Martin Alm, Peter Thomsen, Maisem Laabei, A. Toby A. JenkinsIn silico identification of urease inhibitors based on thiourea, tested to determine IC50 and tested on a catheterised in vitro bladder model, showing efficacy in reducing catheter blockage.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Sidechain structure–activity relationships of cyclobutane-based small molecule αvβ3 antagonists By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3616-3624DOI: 10.1039/D4MD00306C, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Adam Throup, Manar Saleh Zraikat, Andrew Gordon, Shohreh Jafarinejad Soumehsaraei, Kathrin D. Haase, Laurence H. Patterson, Patricia A. Cooper, Katherine Hanlon, Paul M. Loadman, Mark Sutherland, Steven D. Shnyder, Helen M. SheldrakeCyclobutanes provide a versatile scaffold for the synthesis of small molecule integrin antagonists with good metabolic stability and in vivo tolerability.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b A novel, glutathione-activated prodrug of pimasertib loaded in liposomes for targeted cancer therapy By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00517A, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Arianna Amenta, Susanna Comi, Marcelo Kravicz, Silvia Sesana, Antonia Antoniou, Daniele Passarella, Pierfausto Seneci, Sara Pellegrino, Francesca ReA novel, glutathione-activated prodrug of pimasertib (PROPIMA) has been developed. PROPIMA showed ability to inhibit tumour cell migration and proliferation controlled over time, while also achieving a high incorporation rate into liposomes.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Design, synthesis, and structure–activity relationship studies of 6H-benzo[b]indeno[1,2-d]thiophen-6-one derivatives as DYRK1A/CLK1/CLK4/haspin inhibitors By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00537F, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Abdelfattah Faouzi, Alexandre Arnaud, François Hallé, Jean Roussel, Mandy Aymard, Vincent Denavit, Cong Viet Do, Angélique Mularoni, Mohamed Salah, Ahmed ElHady, Thanh-Nhat Pham, Alexandre Bancet, Marc Le Borgne, Raphaël Terreux, Roland Barret, Matthias Engel, Thierry LombergetA series of sulfur-containing tetracycles was designed and evaluated for their ability to inhibit protein kinase DYRK1A, a target known to have several potential therapeutic applications including cancers, Down syndrome or Alzheimer's disease.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00471J, Research ArticlePoorvi Saraf, Bhagwati Bhardwaj, Akash Verma, Mohammad Aquib Siddiqui, Himanshu Verma, Pradeep Kumar, Samridhi Srivastava, Sairam Krishnamurthy, Saripella Srikrishna, Sushant Kumar ShrivastavaScreening piperazine derivatives via ChEMBL database led to the design and synthesis of novel dual COX-2/5-LOX inhibitors with strong anti-inflammatory, analgesic, and anti-cancer activity.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00608A, Research ArticleSunil Kumar, Bishnu Prasad Pandey, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Rania B. Bakr, Hoon Kim, Bijo MathewA total of 18 heterocyclic derived conjugated dienones (CD1–CD18) were evaluated for their potential monoamine oxidase (MAO)-A/-B inhibitory activity.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00297K, Research ArticleBranislava Tenjović, Sofija Bekić, Andjelka Ćelić, Edward Petri, Julia Scholda, Florian Kopp, Marija Sakač, Andrea NikolićIn this study, a series of 13 new D-ring fused steroidal N(2)-substituted-1,2,3-triazoles were synthesized, characterized and evaluated for their biological activities.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Design and Synthesis of coumarin-based amphoteric antimicrobials with the biofilm interference and immunoregulation effects By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00721B, Research ArticleQun Tang, Haiyang Zhang, Kasemsiri Chandarajoti, Zirui Jiao, Lianhua Nie, Sai Lv, Jiakun Zuo, Wen Zhou, Xiangan HanBacterial infections pose a threat to the health of animals and human being, and the biofilm formation exacerbates the microbial threat. New antimicrobial agents to address this challenge are much...The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00662C, Research ArticleRajat Arora, Ayan Mukherjee, Gilbert Arthur, Mark W. Nachtigal, Frank SchweizerWe describe the multi-step synthesis of different dibasic and tribasic galactosamine-based glycosylated antitumor ether lipids (GAELs) and their cytotoxic response in comparison to doxorubicin and cisplatin.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00541D, Research ArticleMikhail N. Anisimov, Maksim A. Boichenko, Vitaly V. Shorokhov, Julia N. Borzunova, Marina Janibekova, Vadim V. Mustyatsa, Ilya A. Lifshits, Andrey Yu. Plodukhin, Ivan A. Andreev, Nina K. Ratmanova, Sergey S. Zhokhov, Elena A. Tarasenko, Daria A. Ipatova, Alexander R. Pisarev, Ivan A. Vorobjev, Igor V. Trushkov, Olga A. Ivanova, Nikita B. GudimchukNew 1,5-disubstituted pyrrolidin-2-ones 1, 2 and 5-aryl-3,3a,4,5-tetrahydropyrrolo[1,2-a]quinoline-1(2H)-ones 3 were explored as inhibitors of tubulin polymerization.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Development, biological evaluation, and molecular modelling of some benzene-sulfonamide derivatives as protein tyrosine phosphatase-1B inhibitors for managing diabetes mellitus and associated metabolic disorders By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00594E, Research ArticleNagat Ghareb, Khaled M. Darwish, Mohamed S. Nafie, Ranwa Elrayess, Noha M. Abourobe, Shaimaa A. Fattah, Reem M. Hazem, Eman T. Mehanna, Ranza ElrayessOne benzene-sulfonamide derivative exhibited potent protein tyrosine phosphatase-1B inhibition for managing diabetes mellitus and associated metabolic disorders.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Correction: Anti-schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD90044H, Correction Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Kennosuke Itoh, Hiroki Nakahara, Atsushi Takashino, Aya Hara, Akiho Katsuno, Yuriko Abe, Takaaki Mizuguchi, Fumika Karaki, Shigeto Hirayama, Kenichiro Nagai, Reiko Seki, Noriko Sato, Kazuki Okuyama, Masashi Hashimoto, Ken Tokunaga, Hitoshi Ishida, Fusako Mikami, Kofi Dadzie Kwofie, Hayato Kawada, Bangzhong Lin, Kazuto Nunomura, Toshio Kanai, Takeshi Hatta, Naotoshi Tsuji, Junichi Haruta, Hideaki FujiiTo cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Breaking boundaries in diabetic nephropathy treatment: design and synthesis of novel steroidal SGLT2 inhibitors By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00645C, Research ArticleGeetmani Singh Nongthombam, Semim Akhtar Ahmed, Kangkon Saikia, Sanjib Gogoi, Jagat Chandra BorahVirtual screening and synthetic modification of natural product-derived steroidal precursors as potential SGLT2 inhibitors for the treatment of diabetic nephropathy.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Human microbiome derived synthetic antimicrobial peptides with activity against Gram-negative, Gram-positive, and antibiotic resistant bacteria By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00383G, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Walaa K. Mousa, Ashif Y. Shaikh, Rose Ghemrawi, Mohammed Aldulaimi, Aya Al Ali, Nour Sammani, Mostafa Khair, Mohamed I. Helal, Farah Al-Marzooq, Emilia OueisAn AMP-derived short 15-mer peptide and its cyclic derivatives have low micromolar broad spectrum antibacterial activity, with rapid onset of bactericidal effect and a membrane-targeting mode of action.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Amides of moronic acid and morolic acid with the tripeptides MAG and GAM targeting antimicrobial, antiviral and cytotoxic effects By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00742E, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Uladzimir Bildziukevich, Lucie Cerna, Jana Trylčová, Marie Kvasnicova, Lucie Rárová, David Šaman, Petra Lovecká, Jan Weber, Zdenek WimmerA series of amides of the selected plant triterpenoids, moronic acid and morolic acid, with the tripeptides MAG and GAM was designed and synthesized. Two required tripeptides 5 and 10...The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Novel benzenesulfonamides containing a dual triazole moiety with selective carbonic anhydrase inhibition and anticancer activity By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00617H, Research ArticleAida Buza, Cüneyt Türkeş, Mustafa Arslan, Yeliz Demir, Busra Dincer, Arleta Rifati Nixha, Şükrü BeydemirIn this research, a series of sulfonamides incorporating a 1,2,3-triazolyloxime substituted 1,2,3-triazolyl moiety was conceptualized, synthesized, and investigated as carbonic anhydrase inhibitors.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Azo derivatives of monoterpenes as anti-Helicobacter pylori agents: from synthesis to structure-based target investigation By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00511B, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Francesco Melfi, Marialuigia Fantacuzzi, Simone Carradori, Ilaria D'Agostino, Alessandra Ammazzalorso, Noemi Mencarelli, Marialucia Gallorini, Mattia Spano, Paolo Guglielmi, Mariangela Agamennone, Sazan Haji Ali, Ali Al-Samydai, Francesca SistoMonoterpene-derived azo benzenes showed selective antibacterial activity against Helicobacter pylori with a safe profile. An in silico investigation highlighted the inosine 5'-monophosphate dehydrogenase enzyme as the putative target.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Medicinal chemistry-based perspective on thiophene and its derivatives: Exploring the structural insights to discover plausible druggable leads By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00450G, Review ArticleShikha Thakur, Devendra Kumar, shivani jaiswal, Kapil Kumar Goel, Pramod Rawat, Vivek Srivastava, Sonia Dhiman, Hemant R Jadhav, Ashish Ranjan DwivediThiophene is a privileged pharmacophore in medicinal chemistry owing to its diversified biological attributes. The thiophene moiety has been ranked 4th in US FDA drug approval of small drug molecules,...The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b A decade of pyridine-containing heterocycles in US FDA approved drugs: a medicinal chemistry-based analysis By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00632A, Review ArticleAshish Ranjan Dwivedi, Shivani Jaiswal, Deepak Kukkar, Roshan Kumar, Thakur Gurjeet Singh, Mahendra Pratap Singh, Abhay M. Gaidhane, Sorabh Lakhanpal, K. Nagendra Prasad, Bhupinder KumarThe present review is a concerted effort to cover drugs bearing pyridine rings approved in the last decade, and it provides thorough discussion and commentary on their pharmacokinetics and pharmacodynamics together with in-depth structural analysis.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00579A, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Cecilia C. Ayala-Aguilera, Yang Ge, Álvaro Lorente-Macías, Benjamin N. Jones, Catherine Adam, Neil O. Carragher, Asier Unciti-BrocetaA ligand-centred strategy combined with phenotypic screening was used to develop novel antiproliferative inhibitors against oesophageal cancer and identified a lead compound that induces potent anticancer activity and inhibits Aurora kinase A.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00621F, Research ArticleChunfei Zhang, Yixin Liu, Xiao Zhang, Chunping Wan, Zewei MaoA series of novel benzofuran-based chalcone derivatives could be considered as potent VEGFR-2 inhibitors.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b S-MGBs bearing amidine tail groups are potent, selective antiplasmodial agents By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00619D, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Marina Perieteanu, Tayner Rodriguez Garzon, Leah M. C. McGee, Abedawn I. Khalaf, Colin J. Suckling, Rebecca Beveridge, Vicky M. Avery, Fraser J. Scott25 S-MGBs, including those bearing an amidine tail group, were investigated for their antiplasmodial, in vitro activity against 3D7 and Dd2 strains of P. falciparum. Several potent, and selective, hit compounds were identified.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 Mpro inhibitors with improved metabolic stability By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00555D, Research ArticleShenghua Gao, Letian Song, Bing Ye, Mianling Yang, Junyi Li, Manyu Gu, Ann E. Tollefson, Karoly Toth, Peng Zhan, Xinyong LiuThe continuous mutational nature of SARS-CoV-2 and its inter-species' similarities emphasize the urgent need to design and develop more direct-acting antiviral agents against highly infectious variants.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Advances in antibacterial agents for Mycobacterium fortuitum By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00508B, Review ArticleCarlos Roberto Tavolari Jortieke, Angélica Rocha Joaquim, Fernando FumagalliThis review presents the recent findings on antibacterial agents against Mycobacterium fortuitum and reveals the most promising and effective chemical frameworks to inspire the development of new drugs.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b A novel approach for the synthesis of the cyclic lipopeptide globomycin By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00685B, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Samantha J. Bann, Stephen A. CochraneLipid swapping: a new approach for the synthesis of globomycin that allows for facile lipid diversification.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Design, synthesis, and biological evaluation of pyrazole–ciprofloxacin hybrids as antibacterial and antibiofilm agents against Staphylococcus aureus By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00623B, Research ArticleOjaswitha Ommi, Priyanka Sudhir Dhopat, Shashikanta Sau, Madhu Rekha Estharla, Srinivas Nanduri, Nitin Pal Kalia, Venkata Madhavi YaddanapudiA series of pyrazole–ciprofloxacin hybrids were designed, synthesized, and tested for antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Mycobacterium tuberculosis, aiming to combat antibiotic resistance.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Novel quinoxaline-derived derivatives: design, synthesis, bioactive evaluation, SARs and preliminary antibacterial mechanism By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00670D, Research ArticleYuting Liu, Pengju Yang, Yunyun Zhou, Zhiwen ZhouIn the current study, we have designed and prepared a series of quinoxaline-based compounds, which were derived from o-phenylenediamine. Among which, compounds 5m-p displayed good to moderate antibacterial activity with...The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Design and synthesis of (E)-3-benzylideneindolin-2-one derivatives as potential allosteric inhibitors of Aurora A kinase By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00373J, Research ArticleYongLai Jiao, Jie Zhong, Jin-Fang Xu, Shaobo Ning, Taigang Liang, Mingzhu Zhao, Jian ZhangThe mitotic kinase Aurora A, a pivotal regulator of cell cycle, is overexpressed in various cancers and has emerged as one of the most promising targets for anticancer drug discovery....The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Enhancing the antimycobacterial efficacy of pyridine-4-carbohydrazide: linkage to additional antimicrobial agents via oxocarboxylic acids By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00663A, Research Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Václav Pflégr, Klára Konečná, Jiřina Stolaříková, Jan Ősterreicher, Ondřej Janďourek, Martin KrátkýLinking pyridine-4-carbohydrazide to other antimicrobial agents via oxocarboxylic acids significantly enhances efficacy against mycobacteria with promising selectivity and safety profiles.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Synthesis of cationic N-acylated thiazolidine for selective activity against Gram-positive bacteria and evaluation of N-acylation's role in membrane-disrupting activity By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00626G, Research ArticleAleena Pious, Vignesh Venkatasubramanian, Dharshini Karnan Singaravelu, Subburethinam Ramesh, Fuad Ameen, Anbazhagan VeerappanLipidation modulates the Gram-selective antibacterial activity of QPyNATh.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Synthesis, in silico and bio-evaluation studies of new isothiocyanate derivatives with respect to COX inhibition and H2S release profiles By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00495G, Research ArticleYakup Berkay Yilmaz, Tuğba Güngör, Serhat Dönmez, Hazal Nazlıcan Atalay, Pınar Siyah, Serdar Durdağı, Mehmet Ay, Tugba Boyunegmez TumerNew isothiocyanate derivatives (I1–3 and I1a–e) were synthesized and screened for their anti-inflammatory activities and H2S-releasing capacities. Compounds I1 and I1c demonstrated the most potent and selective COX-2 inhibition.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00601A, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Brém Balázs, Bianca Stoean (Vasile), Éva Molnár, Eva Fischer-Fodor, Ovidiu Bălăcescu, Raluca Borlan, Monica Focsan, Adriana Grozav, Patriciu Achimaş-Cadariu, Emese Gál, Luiza GainaNew meso-substituted AB3-type phenothiazinyl porphyrins and ferrocenylvinyl phenothiazinyl porphyrin were synthesised by Suzuki–Miyaura and Mizoroki–Heck cross-coupling reactions, respectively.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00553H, Research ArticleStefano Tomassi, Benito Natale, Michele Roggia, Luisa Amato, Caterina De Rosa, Carminia Maria Della Corte, Emma Baglini, Giorgio Amendola, Anna Messere, Salvatore Di Maro, Elisabetta Barresi, Federico Da Settimo, Maria Letizia Trincavelli, Fortunato Ciardiello, Sabrina Taliani, Floriana Morgillo, Sandro CosconatiNon-small cell lung cancer (NSCLC), the leading cause of cancer-related mortality worldwide, poses a formidable challenge due to its heterogeneity and the emergence of resistance to targeted therapies.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00637B, Review Article Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Qiang Yang, Yunpeng LiuFc-glycan-specific ADC is a significant advance in site-specific ADCs for cancer therapy. Notably, JSKN003 and IBI343 have demonstrated promising results in phase 1 clinical trials and are advancing into phase 3 studies.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
b Light enhanced cytotoxicity and antitumoral effect of a ruthenium-based photosensitizer inspired from natural alkaloids By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00600C, Research Article Open Access   This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.Gennaro Sanità, Maria Laura Alfieri, Barbara Carrese, Serena Damian, Vincenza Mele, Gaetano Calì, Brigida Silvestri, Sebastiano Marra, Susan Mohammadi, Giuseppina Luciani, Paola Manini, Annalisa LambertiBiological assays carried out on melanoma and breast cancer cells highlighted the role of light in boosting the cytotoxic effect of a ruthenium complex featuring a dihydroisoquinoline ligand suggesting applications in photodynamic therapy.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article