RSC Medicinal Chemistry Blog

RSC Medicinal Chemistry is delighted to introduce our Editor’s choice collection

This collection showcases some of the best articles published in the journal, handpicked by our Associate Editors and Editorial Board members.

Below we have a selection of recent RSC Medicinal Chemistry articles chosen by Associate Editor Cynthia Dowd (George Washington University, USA). Take a look at which articles he chose and why.

Cynthia Dowd’s favourite articles

Rational design of small-sized peptidomimetic inhibitors disrupting protein–protein interaction Junyuan Wang, Ping Zheng, Jianqiang Yu, Xiuyan Yang* and Jian Zhang* RSC Med. Chem., 2024, 15, 2212-2225

Cynthia’s comments:

“Disruption of protein-protein interfaces could be seen as the ‘holy grail’ of drug discovery. Indeed, much of biology and biochemistry is mediated through such protein-protein interactions (PPI). In this review, Wang et al. describe the most recent strategies for the design and development of molecules aimed at disrupting PPI. These strategies could be used by the field across a variety of protein partners.”

Replacement of nitro function by free boronic acid in non-steroidal anti-androgens (Open Access) Petr Šlechta, Roman Viták, Pavel Bárta, Kateřina Koucká, Monika Berková, Diana Žďárová, Andrea Petríková, Jiří Kuneš, Vladimír Kubíček, Martin Doležal, Radek Kučera and Marta Kučerová-Chlupáčová* RSC Med. Chem., 2024, 15, 4018-4038

Cynthia’s comments:

“Since the clinical introduction and success of bortezomib, the investigation of boron and boronic acids in medicinal chemistry has increased. The work in this paper expands on the exploration of the boronic acid as an isostere of the nitro group within a set of antiandrogens. The authors investigate not only in vitro activity, but also the toxicity of the resulting molecules, enabling expansion of nitro-group isosterism that might be applicable to other compound classes.”

Small molecule antipathogenic agents against Staphylococcus aureus infections Paulo Anastácio Furtado Pacheco, Charlotte Uldahl Jansen, Morten Rybtke, Tim Tolker-Nielsen and Katrine Qvortrup* RSC Med. Chem., 2025, Advance Article

Cynthia’s comments:

“Many anti-infective drug discovery efforts have been focused on inhibition of a function that is essential to the pathogen. In this review, the authors report on work aimed at targeting bacterial virulence factors as a way of controlling the organism. Termed “antipathogenic drugs”, these methods may result in less drug resistance compared with more traditional antibacterial drug discovery.”

Meet the Editor

Cynthia Dowd, RSC Medicinal Chemistry Associate Editor George Washington University, USA Dr. Cynthia Dowd is a Professor of Chemistry at George Washington University.  She obtained a BA in Chemistry from the University of Virginia and a PhD in Medicinal Chemistry from Virginia Commonwealth University.  Following a postdoc at the University of Pennsylvania, Cindy was an intramural scientist at the National Institutes of Health (NIH).  There, she led a small molecule chemistry group to discover novel agents against tuberculosis. In 2007, she began her independent career at GWU where her research is focused on the design and synthesis of novel anti-infective therapies, directed primarily against tuberculosis, malaria and the ESKAPE pathogens.

We hope you enjoyed reading these articles. Keep an eye out on our collection webpage for more of our Editors’ favourite articles.

RSC Medicinal Chemistry is delighted to introduce our Editor’s choice collection

This collection showcases some of the best articles published in the journal, handpicked by our Associate Editors and Editorial Board members.

Below we have a selection of recent RSC Medicinal Chemistry articles chosen by Associate Editor Jian Zhang (Shanghai Jiao Tong University School of Medicine, China). Take a look at which articles he chose and why.

Jian Zhang’s favourite articles

Rosavin improves insulin resistance and alleviates hepatic and kidney damage via modulating the cGAS-STING pathway and autophagy signaling in HFD/STZ-induced T2DM animals Hebatallah S. Ali*, Hiba S. Al-Amodi, Shaimaa Hamady, Marian M. S. Roushdy, Amany Helmy Hasanin, Ghada Ellithy, Rasha A. Elmansy, Hagir H. T. Ahmed, Enshrah M. E. Ahmed, Doaa M. A. Elzoghby, Hala F. M. Kamel, Ghida Hassan, Hind A. ELsawi, Laila M. Farid, Mariam B. Abouelkhair, Eman K. Habib, Mohamed Esawie, Heba Fikry, Lobna A. Saleh and Marwa Matboli* RSC Med. Chem., 2024, 15, 2098-2113

Jian’s comments:

“This research has found that rosavin can improve insulin resistance and alleviate liver and kidney damage, providing experimental evidence for the application of rosavin in the treatment of diabetes. It provides a direction for the development of new diabetes treatment drugs or strategies and has potential clinical application value.”

Exploiting spirooxindoles for dual DNA targeting/CDK2 inhibition and simultaneous mitigation of oxidative stress towards selective NSCLC therapy; synthesis, evaluation, and molecular modelling studies Mohammad Shahidul Islam, Refaah M. Al-Jassas, Abdullah Mohammed Al-Majid*, Matti Haukka, Mohamed S. Nafie, Marwa M. Abu-Serie, Mohamed Teleb*, Amira El-Yazbi, Abdul Majeed Abdullah Alayyaf, Assem Barakat* and Marwa M. Shaaban* RSC Med. Chem., 2024,15, 2937-2958

Jian’s comments:

“Ligand-capped oxindole compounds were designed and studied, which can simultaneously achieve dual DNA targeting, CDK2 inhibition, and reduction of oxidative stress. This provides a multi-targeted treatment strategy for non-small cell lung cancer (NSCLC), potentially overcoming the limitations of single-target treatment and improving the therapeutic effect.”

The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif Ruolin Cao, Fangyu Du, Zhiqiang Liu, Pengcheng Cai, Minggang Qi, Wei Xiao*, Xuefei Bao* and Guoliang Chen* RSC Med. Chem., 2024, 15, 3576-3596

Jian’s comments:

“This paper designed and studied the macrocyclic oxindole compounds, which could simultaneously achieve dual DNA target design and synthesized a ROCK2 inhibitor with a 1, 2-dithia-cyclopentane-3-yl motif. The introduction of this specific structure may provide new ideas and structural templates for the design of ROCK2 inhibitors and enrich the chemical structure diversity of ROCK2 inhibitors.”

Meet the Editor

Jian Zhang, RSC Medicinal Chemistry Associate Editor Shanghai Jiao Tong University School of Medicine, China Jian Zhang is a Distinguished Professor and Head of the Medicinal Chemistry & Bioinformatics Center at Shanghai Jiaotong University School of Medicine. In addition, he is also Dean of the School of Pharmacy at Ningxia Medical University, a member of the Academic Degrees Committee of the State Council in China, and founder of Nutshell Therapeutics. In the last decade, his research has been concerned with drug design, medicinal chemistry and chemical biology, especially target identification and first-in-class allosteric drug discovery.

We hope you enjoyed reading these articles. Keep an eye out on our collection webpage for more of our Editors’ favourite articles.

This article describes the structure-guided optimisation of a screening hit against the pro-survival protein BCL-X_L, which is often overexpressed in solid tumors and results in malignant tumor cells showing resistance to anticancer treatments.

Structure-guided design of a selective BCL-X_L inhibitor
Guillaume Lessene, Peter E Czabotar, Brad E Sleebs, Kerry Zobel, Kym N Lowes, Jerry M Adams, Jonathan B Baell, Peter M Colman, Kurt Deshayes, Wayne J Fairbrother, John A Flygare, Paul Gibbons, Wilhelmus J A Kersten, Sanji Kulasegaram, Rebecca M Moss, John P Parisot, Brian J Smith, Ian P Street, Hong Yang, David C S Huang and Keith G Watson
Nature Chemical Biology, 9, 390–397, (2013)

Editors’ Choice articles are articles identified as being of high potential interest to medicinal chemists, selected from the wider literature by members of the Editorial Board.

In this commentary article, Mark Bunnage and colleagues propose that by developing a ‘chemical probe tool kit’, chemical biology can play a more important part in seeking out potentially relevant targets.

Target validation using chemical probes
Mark E Bunnage, Eugene L Piatnitski Chekler & Lyn H Jones
Nature Chemical Biology, 9, 195–199 (2013)

Editors’ Choice articles are articles identified as being of high potential interest to medicinal chemists, selected from the wider literature by members of the Editorial Board.