RSC Medicinal Chemistry

The many facets of sustainability in medicinal chemistry: our personal experience Sustainability cannot be an afterthought; it must be embedded into every framework of medicinal chemistry. This opinion piece explores how integrating the dual pillars of Green Chemistry and One…

🔓Don't miss this #OpenAccess Opinion article, part of our Sustainable Medicinal Chemistry collection, by @mlbolognesi.bsky.social & co @unibo.it providing their personal experience on the many facets of sustainability in medicinal chemistry #medchem 🧪

Check it out here👇

📢Know someone worthy of the @rscbmcs.bsky.social Hall of Fame?

Nominations are open for the 2026 inductee recognising a prominent chemist for outstanding, sustained contributions to areas of interest to the BMCS #chemsky #chembio #medchem

Find out how to nominate🔽
www.rscbmcs.org/awards/hallo...

N-Cyano sulfoximine-mediated thiazole ligation with N-terminal cysteine under mild aqueous conditions An N-terminal cysteine-selective click reaction employing N-cyano sulfoximines enables rapid thiazole formation under mild conditions. These three-dimensional, hydrophilic scaffolds offer high…

🔓Check out #OpenAccess research from Hwan Jung Lim, Seong Jun Park et al. at KRICT in our latest issue describing N-cyano sulfoximine-mediated thiazole ligation with N-terminal cysteine under mild aqueous conditions #medchem 🧪

Read their full report on our website🔽

Mitochondria-targeting symmetric diiminoguanidines: potent and selective anticancer agents against pancreatic tumors Pancreatic cancer remains one of the deadliest malignancies of the 21st century, with a five-year survival rate below 12%. Its growing incidence is strongly linked to modern lifestyles, marked by…

🔓Take a look in our latest issue at #OpenAccess research by Sigrid Lacaille & Andreea R. Schmitzer reporting mitochondria-targeting symmetric diiminoguanidines as potent and selective anticancer agents against pancreatic tumors #medchem 🧪

📍 @umontreal.ca

An overview of recent advancements in targeted cancer therapies and their potential clinical impact Recent advances in medicine and drug development have significantly changed how cancer is treated. The success of inhibitors like sotorasib and adagrasib has expanded options for targeting once…

Read this review, part of our 5th Anniversary collection, by Shams Aaghaz, Ahmed Kamal et al. at BITS Pilani in our latest issue providing an overview of recent advancements in targeted cancer therapies & their potential clinical impact #medchem 🧪

Find it in full below👇

📢We are delighted to announce our #OpenCall for papers to our Macrocyclic Peptide & Peptidomimetics themed collection #chemsky #medchem

Guest Editors: Sandro Cosconati, Cameron Pye, @danithechemist.bsky.social & Philip Thompson

Deadline: 31st July 2026

Find out more🔽
www.rsc.org/publishing/j...

Synthesis and evaluation of enantiomeric quinoline-2-carboxamides: positron emission tomography imaging agents for the translocator protein The translocator protein (TSPO) is a key biomarker for inflammation. Positron emission tomography (PET) imaging of TSPO has emerged as a valuable tool for investigating multiple disorders throughout…

🔓Don't miss this #OpenAccess paper in our latest issue by @andysuth14.bsky.social & co @uofgchem.bsky.social & @edinburgh-uni.bsky.social on the synthesis of enantiomeric quinoline-2-carboxamides as PET imaging agents for the translocator protein #medchem

Check it out🔽

📢Our latest issue is now online!

Check out the review behind the cover by @sculpturatus.bsky.social & co. at @uarizona.bsky.social looking at the history, synthesis and medicinal use of cantharidin, LB-100, and their analogs #medchem

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Discovery and optimization of pyrrolopyrimidines as highly potent, selective and brain-penetrant LRRK2 inhibitors Leucine-rich repeat kinase 2 (LRRK2) is a promising therapeutic target for Parkinson's disease. We report herein the discovery of pyrrolopyrimidine analogs as potent and selective LRRK2 kinase…

Take a look at research in our latest issue by Jeffrey M. Axten & co. on the discovery and optimization of pyrrolopyrimidines as highly potent, selective and brain-penetrant LRRK2 inhibitors #medchem 🧪

📍 @gsk.bsky.social

Novel small molecule derivatives improve survivability in the cellular model of Huntington's disease via improving mitochondrial fusion Mitochondrial dysfunction is one of the primary cellular conditions involved in developing Huntington's disease (HD) pathophysiology. The accumulation of mutant huntingtin protein with abnormal PolyQ…

Read research reporting how novel small molecule derivatives improve survivability in the cellular model of Huntington's disease via improving mitochondrial fusion by Tanmay Chatterjee, Shuvadeep Maity et al. from BITS Pilani in our latest issue #medchem 🧪

Find in full🔽

Recent advances in the antimicrobial potential of boron cluster compounds Since their discovery in the mid-20th century, inorganic boron clusters such as carboranes, metallacarboranes, and dodecaborates have been investigated for a range of medicinal applications, most…

Don't miss this review in our latest issue by @rutledgends.bsky.social, Louis M. Rendina et al. at @sydney.edu.au highlighting the recent advances and medical chemistry opportunities of boron cluster compounds #medchem 🧪

Check it out in full below👇

Screening apelin analogues and a small molecule agonist as effective cardiovascular therapeutics against reperfusion injury Ischemic reperfusion injury is a major global health threat, with the development of effective therapeutics still urgently needed. While both peptide therapeutics and small-molecule agonists have…

🔓Check out #OpenAccess research by John C. Vederas & co. from @ualberta.bsky.social in our latest issue exploring pharmaceutical potential of retro-inverso apelin peptides, part of our 5th Anniversary collection #medchem 🧪

Find in full on our website🔽

Synthesis and evaluation of lupeol-derived triterpenic azines as potential neuroprotective agents Parkinson's disease (PD) is a progressive neurodegenerative disorder characterized by the selective loss of dopaminergic neurons and the accumulation of α-synuclein aggregates. Current treatments are…

Take a look in our latest issue at research from Natalia P. Alza, María Belén Faraoni et al. describing the synthesis and evaluation of lupeol-derived triterpenic azines as potential neuroprotective agents #medchem 🧪

📍Universidad Nacional del Sur

The structural requirements of 3,5-substituted oxindoles that determine selective AMPK or GSK3β inhibition AMP-activated protein kinase (AMPK) acts as a central cellular sensor at the interface of metabolic and signaling networks, that supports cell survival in energetically unfavorable environments. Due…

🔓Be sure to read this #OpenAccess article from Philip Reigan et al. @cuanschutz.bsky.social investigating the structural requirements of 3,5-substituted oxindoles that determine selective AMPK or GSK3β inhibition #medchem 🧪

Find their full report👇

Peripheral tailoring of pentacene: developing next-generation organic sonosensitizers for cancer sonodynamic therapy Sonodynamic therapy (SDT) is an innovative, non-invasive, and effective method for cancer treatment. However, exploring sonosensitizers with high sonosensitivity and biosafety remains a significant…

Don't miss research by Yu Zhang, Jun Luo & co. at Nanjing University of Science & Technology in our latest issue using peripheral tailoring of pentacene to develop next-generation organic sonosensitizers for cancer sonodynamic therapy #medchem 🧪

Check it out here🔽

Fluorinated pyrimidine 5-carboxamides as potential tools for MERTK targeted fluorine-18-PET-radioligand development MER tyrosine kinase (MERTK) is highly expressed on the protective and reparative phenotype of microglia, which is in response to neuroregeneration following the neuronal damage induced by multiple…

Check out research by Trevor J. Kilpatrick, Jonathan B. Baell et al. from @monashuniversity.bsky.social reporting fluorinated pyrimidine 5-carboxamides as potential tools for MERTK targeted fluorine-18-PET-radioligand development #medchem 🧪

Read in full below👇

Prodrug strategies in developing antiviral nucleoside analogs Prodrug strategies are used to enhance the physicochemical and pharmaceutical properties of drug candidates that may not be suitable for specific delivery or are limited by formulation options. A…

🔓Take a look in our latest issue at this #OpenAccess review by Franck Amblard, Raymond Schinazi & co. providing an overview of prodrug strategies in developing antiviral nucleoside analogs #medchem 🧪

📍Emory University

Diversifying the triquinazine scaffold of a Janus kinase inhibitor The exploration of novel three-dimensional scaffolds remains essential for expanding chemical space and discovering new bioactive molecules. Here, we describe a robust synthetic strategy that enables…

🔓Be sure to read #OpenAccess research, part of our 5th Anniversary collection, from Jean-Louis Reymond et al. @reymondgroup.bsky.social at @unibe.ch in our latest issue diversifying the triquinazine scaffold of a Janus kinase inhibitor #medchem 🧪

Find the full report👇

Recent advances in glutarimide chemistry for cereblon-mediated targeted protein degradation: developments in synthesis and diversification The field of targeted protein degradation has garnered significant attention over the past two decades, highlighted by the FDA approval of several therapeutics and the entry of numerous drug…

Don't miss this review in our latest issue by Natalie Holmberg-Douglas & co. @bristolmyerssquibb.bsky.social looking at the recent advances in glutarimide chemistry for cereblon-mediated targeted protein degradation #medchem 🧪

Check it out in full here🔽

📢Our first issue of 2026 is now online!

🔓Check out the #OpenAccess article behind the cover by Naoko Yoshizawa-Sugata, Hisao Masai, Yoko Yamakoshi & co. @ethz.ch reporting new water-soluble cationic porphyrins with enhanced phototoxicity to cancer cell lines #medchem

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Investigating the role of cytochrome bd oxidases in the antibacterial activity of madecassic acid and derivatives thereof Natural products are valuable starting points for drug discovery, although individual modes of action are often difficult to pin down. Ursanes such as madecassic acid have been shown to have antibacte...

Here is our exciting new work on madecassic acid inhibiting bacterial respiration @kent.ac.uk @cjserpell.bsky.social @rscmedchem.rsc.org
doi.org/10.1039/D5MD...

Fantastic line up at the “34th GP2A 2026 Conference on Medicinal Chemistry 2026” #GP2A2026 in Gothenburg, Sweden from 26th- 28th of August 2026. Registration will open soon at the end of January 2026. #MedChem #ChemBio #youngresearcher @naturvetenskap.bsky.social

An innovative strategy to treat pathogenic biofilm-associated infections in vitro and in vivo using guanidinium-linked neomycin lipidation To overcome neomycin's limited efficacy against complex Gram-positive and Gram-negative co-infections, we have developed a novel guanidinium-linked neomycin–lipid conjugate (guanidino Neo-lipid).…

Take a look at recent work by Jhuma Bhadra, Santanu Bhattacharya and colleagues where they present a promising therapeutic strategy for treating persistent infections caused by both Gram-positive and Gram-negative pathogens, including co-infective scenarios👏

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📍IACS 🧪

Discovery of a first-in-class SLIT2 binder disrupting the SLIT2/ROBO1 axis via DNA-encoded library (DEL) screening The SLIT2/ROBO1 signaling axis plays a critical role in neural development, immune regulation, and tumor progression, including glioblastoma. However, small molecule inhibitors targeting this…

🔓Don't miss this #OpenAccess work by Moustafa T. Gabr & co on the discovery of a first-in-class SLIT2 binder disrupting the SLIT2/ROBO1 axis via DNA-encoded library screening⬇️

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📍 @weillcornell.bsky.social 🧪

Data-driven assessment of bioisosteric replacements and their influence on off-target activity profiles Bioisosterism, a fundamental concept in medicinal chemistry, involves the substitution of chemical groups with structural analogs that preserve similar physicochemical properties while potentially…

🔓Don't miss this #OpenAccess article by @gerhardecker.bsky.social and colleagues, using KNIME and ChEMBL data to show how common bioisosteric swaps predictably shift off‑target potencies 👇

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📍 @univie.ac.at 🧪

Targeting clathrin-mediated endocytosis: recent advances in inhibitor development, mechanistic insights, and therapeutic prospects Clathrin-mediated endocytosis (CME) is a critical pathway for cellular uptake of metabolites, hormones, and pathogens, including viruses. Recent advances in understanding CME mechanisms and…

Explore this Review by Jialin Guo, Chun Hu, Junhai Xiao & co discussing the recent progress in finding inhibitors targeting clathrin-mediated endocytosis👏

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📍State Key Laboratory of National Security Specially Needed Medicines & Shenyang Pharmaceutical University 🧪

Sequence-controlled peptoid hydrogels for neuronal trans-differentiation: a synthetic biomaterials approach in future neuroregenerative research Peptide-based hydrogels stimulate stem cell differentiation into neurons, improve neuroprotection, and aid in spinal cord/brain injury repair by moderating inflammatory responses and activating…

🔓Read this #OpenAccess Opinion article by Prabir Kumar Gharai & co on how the use of peptoid-based hydrogels could progress neuroregenerative therapies💡

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📍 @okstate.edu 🧪

RSC Medicinal Chemistry inside front cover for vol 16, issue 12.

Our inside front cover is work by Renato J. S. Oliveira, Dennis Russowsky & co on synthesising fluorescent dihydropyridine–dihydropyrimidinone hybrids and their inhibition of protein kinases for anticancer applications, take a look⬇️

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📍UFRGS and Barretos Cancer Hospital🧪

RSC Medicinal Chemistry outside front cover for vol 16, issue 12.

This month's front cover showcases a Review article by Paul Groundwater & co discussing structural qualities of β-lactamase enzymes and the efficacy of emerging β-lactamase inhibitors against clinically significant carbapenemases, read it here👀

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📍 @sydney.edu.au 🧪

RSC Medicinal Chemistry outside front cover for vol 16, issue 12.

RSC Medicinal Chemistry inside front cover for vol 16, issue 12.

📢Our last issue of 2025 is now online! Read it here👇

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