b

Alia-Ranbir's Daughter Raha Turns 2

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.




b

Why Abhishek Missed Aishwarya's Birthday

When Aishwarya celebrated her birthday in Dubai on November 1, the speculation regarding the Abhishek-Aishwarya marital rift ran even higher.




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

RSC Med. Chem., 2024, 15,3395-3417
DOI: 10.1039/D4MD00334A, Research Article
Vu Ngoc Toan, Do Son Hai, Hoang Thi Kim Van, Nguyen Minh Tri, Duong Ngoc Toan, Nguyen Thi Thanh Mai, Nguyen Dinh Thanh
D-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.
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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

RSC Med. Chem., 2024, 15,3495-3506
DOI: 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. Russell
The 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




b

Integrating amino acids into Bcr-Abl inhibitors: design, synthesis, biological evaluation, and in silico studies

RSC Med. Chem., 2024, 15,3507-3528
DOI: 10.1039/D4MD00417E, Research Article
Yuying Liu, Zeyu Yang, Jie Zhang, Na Guo, Nanxin Liu, Qingqing Zhang, Xintao Dang, Yanchen Li, Jie Zhang, Xiaoyan Pan
In 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




b

The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif

RSC Med. Chem., 2024, 15,3576-3596
DOI: 10.1039/D4MD00438H, Research Article
Ruolin Cao, Fangyu Du, Zhiqiang Liu, Pengcheng Cai, Minggang Qi, Wei Xiao, Xuefei Bao, Guoliang Chen
Rho-associated coiled-coil containing kinase (ROCK) plays an important role in inflammation.
The content of this RSS Feed (c) The Royal Society of Chemistry




b

Discovery of highly potent SARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides

RSC Med. Chem., 2024, 15,3469-3476
DOI: 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 Nencka
SARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides.
The content of this RSS Feed (c) The Royal Society of Chemistry




b

Synthesis and cytotoxic activity of madecassic acid–silybin conjugate compounds in liver cancer cells

RSC Med. Chem., 2024, 15,3418-3432
DOI: 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 Tran
Madecassic 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




b

Synthesis of a celastrol derivative as a cancer stem cell inhibitor through regulation of the STAT3 pathway for treatment of ovarian cancer

RSC Med. Chem., 2024, 15,3433-3443
DOI: 10.1039/D4MD00468J, Research Article
Meijuan Liu, Na Li, Zhaoxue Wang, Shuo Wang, Shaoda Ren, Xiaojing Li
A 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




b

Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation

RSC Med. Chem., 2024, 15,3529-3557
DOI: 10.1039/D4MD00481G, Research Article
Mohamed 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 Adel
Discovery of novel pyridazinone derivatives with dual antimicrobial and anticancer activities.
The content of this RSS Feed (c) The Royal Society of Chemistry




b

Design, synthesis and biological evaluation of a novel PSMA–PI3K small molecule drug conjugate

RSC Med. Chem., 2024, 15,3485-3494
DOI: 10.1039/D4MD00246F, Research Article
Shouguo Peng, Haixia Li, Weilu Cui, Tianning Xiong, Jiaqi Hu, Haixiang Qi, Songwen Lin, Deyu Wu, Ming Ji, Heng Xu
A 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




b

Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists

RSC Med. Chem., 2024, 15,3477-3484
DOI: 10.1039/D4MD00266K, Research Article
Raitis Bobrovs, Svetlana Terentjeva, Ninni Elise Olafsen, Zilvinas Dambrauskas, Antanas Gulbinas, Toivo Maimets, Indrek Teino, Aigars Jirgensons, Jason Matthews, Kristaps Jaudzems
The 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




b

Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019–2024)

RSC Med. Chem., 2024, 15,3371-3394
DOI: 10.1039/D4MD00384E, Review Article
Debasis Das, Lingzhi Xie, Jian Hong
Prospects 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




b

Rationally modified SNX-class Hsp90 inhibitors disrupt extracellular fibronectin assembly without intracellular Hsp90 activity

RSC Med. Chem., 2024, 15,3609-3615
DOI: 10.1039/D4MD00501E, Research Article
Open Access
Gciniwe S. Mathenjwa, Abir Chakraborty, Abantika Chakraborty, Ronel Muller, Mathew P. Akerman, Moira L. Bode, Adrienne L. Edkins, Clinton G. L. Veale
Rationally 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




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.

RSC Med. Chem., 2024, 15,3558-3575
DOI: 10.1039/D4MD00391H, Research Article
Pothiyil S. Vimalkumar, Neethu Sivadas, Vishnu Priya Murali, Daisy R. Sherin, Madhukrishnan Murali, Anuja Gracy Joseph, Kokkuvayil Vasu Radhakrishnan, Kaustabh Kumar Maiti
Malabaricone 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




b

Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage

RSC Med. Chem., 2024, 15,3597-3608
DOI: 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. Jenkins
In 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




b

Sidechain structure–activity relationships of cyclobutane-based small molecule αvβ3 antagonists

RSC Med. Chem., 2024, 15,3616-3624
DOI: 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. Sheldrake
Cyclobutanes 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




b

A novel, glutathione-activated prodrug of pimasertib loaded in liposomes for targeted cancer therapy

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00517A, Research Article
Open Access
Arianna Amenta, Susanna Comi, Marcelo Kravicz, Silvia Sesana, Antonia Antoniou, Daniele Passarella, Pierfausto Seneci, Sara Pellegrino, Francesca Re
A 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.
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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

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00537F, Research Article
Open Access
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 Lomberget
A 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.
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b

Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00471J, Research Article
Poorvi Saraf, Bhagwati Bhardwaj, Akash Verma, Mohammad Aquib Siddiqui, Himanshu Verma, Pradeep Kumar, Samridhi Srivastava, Sairam Krishnamurthy, Saripella Srikrishna, Sushant Kumar Shrivastava
Screening 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.
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b

Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00608A, Research Article
Sunil Kumar, Bishnu Prasad Pandey, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Rania B. Bakr, Hoon Kim, Bijo Mathew
A total of 18 heterocyclic derived conjugated dienones (CD1–CD18) were evaluated for their potential monoamine oxidase (MAO)-A/-B inhibitory activity.
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b

Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00297K, Research Article
Branislava Tenjović, Sofija Bekić, Andjelka Ćelić, Edward Petri, Julia Scholda, Florian Kopp, Marija Sakač, Andrea Nikolić
In 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.
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b

Design and Synthesis of coumarin-based amphoteric antimicrobials with the biofilm interference and immunoregulation effects

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00721B, Research Article
Qun Tang, Haiyang Zhang, Kasemsiri Chandarajoti, Zirui Jiao, Lianhua Nie, Sai Lv, Jiakun Zuo, Wen Zhou, Xiangan Han
Bacterial 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




b

Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00662C, Research Article
Rajat Arora, Ayan Mukherjee, Gilbert Arthur, Mark W. Nachtigal, Frank Schweizer
We 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.
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b

Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00541D, Research Article
Mikhail 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. Gudimchuk
New 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.
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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

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00594E, Research Article
Nagat Ghareb, Khaled M. Darwish, Mohamed S. Nafie, Ranwa Elrayess, Noha M. Abourobe, Shaimaa A. Fattah, Reem M. Hazem, Eman T. Mehanna, Ranza Elrayess
One benzene-sulfonamide derivative exhibited potent protein tyrosine phosphatase-1B inhibition for managing diabetes mellitus and associated metabolic disorders.
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b

Correction: Anti-schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis

RSC Med. Chem., 2024, Advance Article
DOI: 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 Fujii
To cite this article before page numbers are assigned, use the DOI form of citation above.
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b

Breaking boundaries in diabetic nephropathy treatment: design and synthesis of novel steroidal SGLT2 inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00645C, Research Article
Geetmani Singh Nongthombam, Semim Akhtar Ahmed, Kangkon Saikia, Sanjib Gogoi, Jagat Chandra Borah
Virtual screening and synthetic modification of natural product-derived steroidal precursors as potential SGLT2 inhibitors for the treatment of diabetic nephropathy.
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b

Human microbiome derived synthetic antimicrobial peptides with activity against Gram-negative, Gram-positive, and antibiotic resistant bacteria

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00383G, Research Article
Open Access
Walaa K. Mousa, Ashif Y. Shaikh, Rose Ghemrawi, Mohammed Aldulaimi, Aya Al Ali, Nour Sammani, Mostafa Khair, Mohamed I. Helal, Farah Al-Marzooq, Emilia Oueis
An 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.
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b

Amides of moronic acid and morolic acid with the tripeptides MAG and GAM targeting antimicrobial, antiviral and cytotoxic effects

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 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 Wimmer
A 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




b

Novel benzenesulfonamides containing a dual triazole moiety with selective carbonic anhydrase inhibition and anticancer activity

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00617H, Research Article
Aida Buza, Cüneyt Türkeş, Mustafa Arslan, Yeliz Demir, Busra Dincer, Arleta Rifati Nixha, Şükrü Beydemir
In 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.
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b

Azo derivatives of monoterpenes as anti-Helicobacter pylori agents: from synthesis to structure-based target investigation

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00511B, Research Article
Open Access
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 Sisto
Monoterpene-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.
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b

Medicinal chemistry-based perspective on thiophene and its derivatives: Exploring the structural insights to discover plausible druggable leads

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00450G, Review Article
Shikha Thakur, Devendra Kumar, shivani jaiswal, Kapil Kumar Goel, Pramod Rawat, Vivek Srivastava, Sonia Dhiman, Hemant R Jadhav, Ashish Ranjan Dwivedi
Thiophene 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,...
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b

A decade of pyridine-containing heterocycles in US FDA approved drugs: a medicinal chemistry-based analysis

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00632A, Review Article
Ashish Ranjan Dwivedi, Shivani Jaiswal, Deepak Kukkar, Roshan Kumar, Thakur Gurjeet Singh, Mahendra Pratap Singh, Abhay M. Gaidhane, Sorabh Lakhanpal, K. Nagendra Prasad, Bhupinder Kumar
The 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.
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b

Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00579A, Research Article
Open Access
Cecilia C. Ayala-Aguilera, Yang Ge, Álvaro Lorente-Macías, Benjamin N. Jones, Catherine Adam, Neil O. Carragher, Asier Unciti-Broceta
A 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.
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b

Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00621F, Research Article
Chunfei Zhang, Yixin Liu, Xiao Zhang, Chunping Wan, Zewei Mao
A series of novel benzofuran-based chalcone derivatives could be considered as potent VEGFR-2 inhibitors.
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b

S-MGBs bearing amidine tail groups are potent, selective antiplasmodial agents

RSC Med. Chem., 2024, Advance Article
DOI: 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. Scott
25 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.
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b

Miniaturized click chemistry and direct screening facilitate the discovery of triazole piperazine SARS-CoV-2 Mpro inhibitors with improved metabolic stability

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00555D, Research Article
Shenghua Gao, Letian Song, Bing Ye, Mianling Yang, Junyi Li, Manyu Gu, Ann E. Tollefson, Karoly Toth, Peng Zhan, Xinyong Liu
The 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.
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b

Advances in antibacterial agents for Mycobacterium fortuitum

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00508B, Review Article
Carlos Roberto Tavolari Jortieke, Angélica Rocha Joaquim, Fernando Fumagalli
This 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.
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b

A novel approach for the synthesis of the cyclic lipopeptide globomycin

RSC Med. Chem., 2024, Advance Article
DOI: 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. Cochrane
Lipid swapping: a new approach for the synthesis of globomycin that allows for facile lipid diversification.
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b

Design, synthesis, and biological evaluation of pyrazole–ciprofloxacin hybrids as antibacterial and antibiofilm agents against Staphylococcus aureus

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00623B, Research Article
Ojaswitha Ommi, Priyanka Sudhir Dhopat, Shashikanta Sau, Madhu Rekha Estharla, Srinivas Nanduri, Nitin Pal Kalia, Venkata Madhavi Yaddanapudi
A 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.
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b

Novel quinoxaline-derived derivatives: design, synthesis, bioactive evaluation, SARs and preliminary antibacterial mechanism

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00670D, Research Article
Yuting Liu, Pengju Yang, Yunyun Zhou, Zhiwen Zhou
In 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...
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b

Design and synthesis of (E)-3-benzylideneindolin-2-one derivatives as potential allosteric inhibitors of Aurora A kinase

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00373J, Research Article
YongLai Jiao, Jie Zhong, Jin-Fang Xu, Shaobo Ning, Taigang Liang, Mingzhu Zhao, Jian Zhang
The 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....
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b

Enhancing the antimycobacterial efficacy of pyridine-4-carbohydrazide: linkage to additional antimicrobial agents via oxocarboxylic acids

RSC Med. Chem., 2024, Advance Article
DOI: 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 Krátký
Linking pyridine-4-carbohydrazide to other antimicrobial agents via oxocarboxylic acids significantly enhances efficacy against mycobacteria with promising selectivity and safety profiles.
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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

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00626G, Research Article
Aleena Pious, Vignesh Venkatasubramanian, Dharshini Karnan Singaravelu, Subburethinam Ramesh, Fuad Ameen, Anbazhagan Veerappan
Lipidation modulates the Gram-selective antibacterial activity of QPyNATh.
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b

Synthesis, in silico and bio-evaluation studies of new isothiocyanate derivatives with respect to COX inhibition and H2S release profiles

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00495G, Research Article
Yakup Berkay Yilmaz, Tuğba Güngör, Serhat Dönmez, Hazal Nazlıcan Atalay, Pınar Siyah, Serdar Durdağı, Mehmet Ay, Tugba Boyunegmez Tumer
New 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.
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b

meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00601A, Research Article
Open Access
Brém Balázs, Bianca Stoean (Vasile), Éva Molnár, Eva Fischer-Fodor, Ovidiu Bălăcescu, Raluca Borlan, Monica Focsan, Adriana Grozav, Patriciu Achimaş-Cadariu, Emese Gál, Luiza Gaina
New meso-substituted AB3-type phenothiazinyl porphyrins and ferrocenylvinyl phenothiazinyl porphyrin were synthesised by Suzuki–Miyaura and Mizoroki–Heck cross-coupling reactions, respectively.
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b

Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00553H, Research Article
Stefano 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 Cosconati
Non-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.
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b

Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00637B, Review Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Qiang Yang, Yunpeng Liu
Fc-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.
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b

Light enhanced cytotoxicity and antitumoral effect of a ruthenium-based photosensitizer inspired from natural alkaloids

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00600C, Research Article
Open Access
Gennaro Sanità, Maria Laura Alfieri, Barbara Carrese, Serena Damian, Vincenza Mele, Gaetano Calì, Brigida Silvestri, Sebastiano Marra, Susan Mohammadi, Giuseppina Luciani, Paola Manini, Annalisa Lamberti
Biological 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.
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