io SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3460-3468DOI: 10.1039/D4MD00405A, Research ArticleXiaoqin Luo, Jin Wang, Ruichang Wang, Jiabing Lian, Mengnan Guo, Hongrui Zhou, Mengxue Zhang, Zhe Yang, Xiaolong Li, Xianran He, Xiuli BiSchematic of proposed mechanism for the treatment of the SLL-1A-16 inhibiting the proliferation in NSCLC.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
io 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
io 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
io 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
io 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
io 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
io 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
io 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
io Exploring 7β-amino-6-nitrocholestens as COVID-19 antivirals: in silico, synthesis, evaluation, and integration of artificial intelligence (AI) in drug design: assessing the cytotoxicity and antioxidant activity of 3β-acetoxynitrocholestane By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00257A, Research Article Shahabuddin, Uzma, Mohammad Azam, Mehtab Parveen, Nurul Huda Abd Kadir, Kim Min, Mahboob AlamIn light of the ongoing pandemic caused by SARS-CoV-2, effective and clinically translatable treatments are desperately needed for COVID-19 and its emerging 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
io 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
io Introduction to the themed collection on ‘AI in Medicinal Chemistry’ By pubs.rsc.org Published On :: RSC Med. Chem., 2024, 15,3284-3285DOI: 10.1039/D4MD90035A, EditorialJian Zhang, Ola Engkvist, Gerhard HesslerJian Zhang, Ola Engkvist and Gerhard Hessler introduce the RSC Medicinal Chemistry themed collection on ‘AI in Medicinal Chemistry’.The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
io 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
io 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
io 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
io Therapeutic upregulation of DNA repair pathways: strategies and small molecule activators By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00673A, Review ArticleJuhyung Song, Cheoljun Park, Francis E. B. Cabanting, Yong Woong JunPotential therapeutic target proteins for upregulating DNA repair system are reviewed, along with reported small-molecule activators.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
io 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
io Introduction to the themed collection in honour of Professor Christian Leumann By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD90039A, EditorialMarcel Hollenstein, Eugen StulzMarcel Hollenstein and Eugen Stulz introduce the cross-journal themed collection celebrating Christian Leumann’s retirement.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
io 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
io 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
io 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
io 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
io 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
io 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
io 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
io 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
io 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
io 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
io Metal-free synthesis of N-fused quinazolino-quinazoline-diones as a MALAT1 RNA triple helix intercalator By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00614C, Research ArticleVijay Babu Pathi, Pranotosh Das, Abhyuday Guin, Manish Debnath, Biswadip BanerjiThe development of chemical scaffolds that target highly conserved MALAT1 RNA received attention due to its significance in splicing, nuclear organization, and gene expression in disease progression pathways.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
io 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
io 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
io 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
io Generation and capture of naphthoquinonynes: a new frontier in the development of trypanocidal quinones via aryne chemistry By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00558A, Research ArticleLaura P. R. Figueroa, Renato L. de Carvalho, Renata G. Almeida, Esther R. S. Paz, Emilay B. T. Diogo, Maria H. Araujo, Warley S. Borges, Victor F. S. Ramos, Rubem F. S. Menna-Barreto, James M. Wood, John F. Bower, Eufrânio N. da Silva JúniorThis article presents A-ring functionalized quinones via a modern and efficient new strategy involving the generation and capture of benzyne quinones and their evaluation against Trypanosoma cruzi.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
io Property-based optimisation of PROTACs By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00769G, OpinionJames Scott, Iacovos Michaelides, Markus SchadePROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical...The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
io 3-Thio-3,4,5-Trisubstituted-1,2,4-Triazoles: High Affinity Somatostatin Receptor-4 Agonist Synthesis and Structure-Activity Relationships By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00597J, Research ArticleAlbert Michael Crider, Audrey Hospital, Karin Sandoval, William Neumann, Stephen Kukielski, Lejla Garic, Kristen Ingold, Matthew Dunahoo, Khush Srabony, Rafael Frare, Olivia Slater, Nathan Peel, Maria Kontoyianni, Ken WittSomatostatin receptor-4 (SST4) is a therapeutic target for several conditions, including Alzheimer’s disease, seizures, neuropsychiatric disorders, and pain. Our previous work on 1,2,4-triazole derivatives led to enhanced SST4 binding affinity,...The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
io A practical guide for the assay-dependent characterisation of irreversible inhibitors By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00707G, Review ArticleLavleen K. Mader, Jessica E. Borean, Jeffrey W. KeillorKinetic evaluations for assay dependent characterization of irreversible 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
io SIGMAP: an explainable artificial intelligence tool for SIGMA-1 receptor affinity Prediction By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Accepted ManuscriptDOI: 10.1039/D4MD00722K, Research Article Open Access This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Maria Cristina Lomuscio, Nicola Corriero, Vittoria Nanna, Antonio Piccinno, Michele Saviano, Rosa Lanzilotti, Carmen Abate, Domenico Alberga, Giuseppe Felice MangiatordiDeveloping sigma-1 receptor (S1R) modulators is considered a valuable therapeutic strategy to counteract neurodegeneration, cancer progression, and viral infections, including COVID-19. In this context, in-silico tools capable of accurately predicting...The content of this RSS Feed (c) The Royal Society of Chemistry Full Article
io Synthesis and antifungal evaluation of new azole derivatives containing 1,2,3-triazole By pubs.rsc.org Published On :: RSC Med. Chem., 2024, Advance ArticleDOI: 10.1039/D4MD00724G, Research ArticleZhengxiao Huang, Hongjie Chen, Xiao Zhang, Ruirui Wang, Chunyan Hu, Zewei MaoA series of novel azole derivatives containing 1,2,3-triazole have been synthesized with good antifungal effects on sensitive and drug-resistant C. albicans.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
io Changes in train services notified due to demolition of old bridge near Tiruchi junction By www.thehindu.com Published On :: Tue, 05 Nov 2024 17:30:53 +0530 Full Article Tiruchirapalli
io Will decide on sharing stage with actor Vijay in consultation with VCK leaders: Thirumavalavan By www.thehindu.com Published On :: Tue, 05 Nov 2024 17:44:09 +0530 Mr. Thirumavalavan told reporters in Tiruchi that the book release event was not something that was planned recently, and that he had consented to take part in it almost a year ago Full Article Tamil Nadu
io Duo arrested for possession of banned tobacco products worth ₹3 lakh in Tiruchi By www.thehindu.com Published On :: Wed, 06 Nov 2024 18:23:30 +0530 Full Article Tiruchirapalli
io Ensure time-bound implementation of development schemes, says Thirumavalavan By www.thehindu.com Published On :: Wed, 06 Nov 2024 18:29:00 +0530 Full Article Tiruchirapalli
io Paddy crop loss compensation pegged at ₹36,500 By www.thehindu.com Published On :: Wed, 06 Nov 2024 18:53:01 +0530 Full Article Tiruchirapalli
io TNSTC Kumbakonam Division mops up ₹17.13 crore in four days By www.thehindu.com Published On :: Wed, 06 Nov 2024 18:59:26 +0530 Full Article Tiruchirapalli
io Pumping stations to be set up in eight low-lying areas in Tiruchi to prevent inundation By www.thehindu.com Published On :: Wed, 06 Nov 2024 19:30:58 +0530 Full Article Tiruchirapalli
io Farmers demand withdrawal of Tamil Nadu Land Consolidation Act By www.thehindu.com Published On :: Thu, 07 Nov 2024 17:59:18 +0530 The Coordination Committee of All Farmers’ Associations of Tamil Nadu says the State government has created a situation where industries can acquire fertile lands Full Article Tiruchirapalli
io Udhayanidhi lays foundation stone for infrastructure development projects in Thanjavur district By www.thehindu.com Published On :: Thu, 07 Nov 2024 18:48:04 +0530 Buildings at the Government Arts and Science College, Thirukkattupalli, construction of compound wall and an indoor stadium at the Government Rajah Serfoji College, Thanjavur, are among the projects Full Article Tiruchirapalli
io Bids invited for setting up International Dugong Conservation Centre at Manora By www.thehindu.com Published On :: Thu, 07 Nov 2024 19:03:19 +0530 The proposed centre, to be set up at an estimate of ₹41 crore, is being established to conserve endangered Dugong species and its habitat in the Palk Bay Full Article Tiruchirapalli
io Tiruchi Corporation embarks on special drive at night to capture and sterilise street dogs By www.thehindu.com Published On :: Thu, 07 Nov 2024 19:10:58 +0530 About 125 stray dogs have been caught and sterilised at Tiruchi animal birth control centres in the last 10 days after the Corporation launched the special drive Full Article Tiruchirapalli
io Peravurani farmers’ market starts functioning By www.thehindu.com Published On :: Fri, 08 Nov 2024 18:46:38 +0530 Full Article Tiruchirapalli
io Guidelines issued for fertilizer distribution in Karaikal for samba, thaladi paddy cultivation By www.thehindu.com Published On :: Fri, 08 Nov 2024 19:25:49 +0530 Full Article Tiruchirapalli
