Chiara Borsari

Chemoenzymatic Synthesis of Chiral Piperidines Using the Immobilized Transaminase ATA‐117 in Continuous Flow Reactors

Sara Vicinanza, Ilaria Magrini Alunno, Stefania Patti, Morena Pirotta et autres

Nowadays, there is a growing need for streamlined and sustainable strategies to access chiral nitrogen heterocycles, whose stereodefined frameworks underpin their broad functional and pharmaceutical relevance. Herein, we report a robust continuous flow enzymatic protocol for the stereoselective synthesis of the natural …

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First-in-Class Covalent Inhibitors of PFKFB3: Discovery and Characterization in PDAC Models

Alessandra Fiore, Antônio Scarano, Giulia Antonini, Alexandra Ioana Corfu et autres

Abstract Pancreatic ductal adenocarcinoma (PDAC) is an aggressive cancer, driven by metabolic reprogramming. Since direct glycolytic enzyme inhibition is limited by toxicity, indirect glycolysis modulation through inhibition of the kinase activity of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) may offer a safer therapeutic strategy. Herein, …

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Targeting ALDH7A1 with covalent inhibitors reveals new chemical space for prostate cancer therapy

Raffaella Gallo, Antônio Scarano, Eleonora Gianquinto, Gaia Franzini et autres

Prostate cancer (PCa) remains a major global health burden. Although androgen deprivation and receptor-targeted therapies initially benefit patients, resistance often leads to metastatic castration-resistant prostate cancer, with limited treatment options. Aldehyde dehydrogenase 7A1 (ALDH7A1) is an emerging oncogenic driver of PCa, but …

Targeting ALDH7A1 with covalent inhibitors reveals new chemical space for prostate cancer therapy

Raffaella Gallo, Antônio Scarano, Eleonora Gianquinto, Gaia Franzini et autres

Prostate cancer (PCa) remains a major global health burden. Although androgen deprivation and receptor-targeted therapies initially benefit patients, resistance often leads to metastatic castration-resistant prostate cancer, with limited treatment options. Aldehyde dehydrogenase 7A1 (ALDH7A1) is an emerging oncogenic driver of PCa, but …

Targeting ALDH7A1 with covalent inhibitors reveals new chemical space for prostate cancer therapy

Raffaella Gallo, Antônio Scarano, Eleonora Gianquinto, Gaia Franzini et autres

Prostate cancer (PCa) remains a major global health burden. Although androgen deprivation and receptor-targeted therapies initially benefit patients, resistance often leads to metastatic castration-resistant prostate cancer, with limited treatment options. Aldehyde dehydrogenase 7A1 (ALDH7A1) is an emerging oncogenic driver of PCa, but …

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Fifteen Years, One Mission: Innovative, Inspirational, and Impactful Discoveries

Simone V. Bigi-Botterill, Chiara Borsari, Amanda W. Dombrowski, Michelle A. Estrada et autres

Recommendations F ifteen years ago, the American Chemical Society (ACS) introduced ACS Medicinal Chemistry Letters as a new means to rapidly report new findings in medicinal chemistry.In the inaugural issue of ACS Medicinal Chemistry Letters, the journal's founding Editor-in-Chief, Dennis Liotta, invited …

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From pan-active to parasite-selective antiparasitic agents: A scaffold hopping approach

Chiara Borsari, Nuno Santarém, Dina Coertzen, Asia Mazzolari et autres

Vector-borne parasitic diseases (VBPDs) represent a major global public health concern, with human African trypanosomiasis (HAT), Chagas disease, leishmaniasis, and malaria collectively threatening millions of people, particularly in developing regions. Climate change may further influence their transmission and geographic spread, increasing the …

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Announcing the Early Career Board of Journal of Medicinal Chemistry

Chiara Borsari, Samuele Cazzamalli, John Chu, Yoonji Lee et autres

T he Journal of Medicinal Chemistry is a highly regarded scientific journal that covers a wide array of aspects within medicinal chemistry.Since its inception, it has served as a premier platform for researchers to publish their work on compound design, optimization, and …

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Cover Feature: The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Hit to Lead (ChemMedChem 8/2025)

Jean Quancard, Anders Bach, Chiara Borsari, Russell Craft et autres

“Searching for diamonds in the rough” summarises consensus best practices in how to expedite the processes and enable decision making in the Hits-to-Leads phase of drug discovery. The EFMC Best Practices Group, led by Jean Quancard, draws on expertise from seasoned drug …

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Two-Step Flow Amidation of Natural Phenolic Acids as Antiradical and Antimicrobial Agents

Desirèe Pecora, Sara Vicinanza, Francesca Annunziata, Salvatore Princiotto et autres

High Resolution Image Download MS PowerPoint Slide Natural hydroxycinnamic acid amides (HCAAs) and riparins offer significant health benefits. However, their extraction from natural sources is difficult, and traditional synthetic methods remain wasteful, raising the need for more efficient alternatives. In this work, …

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The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Hit to Lead

Jean Quancard, Anders Bach, Chiara Borsari, Russell Craft et autres

The Hit to Lead (H2L) process is an integral part of contemporary drug discovery, encompassing the optimisation of validated Hit structures into Lead molecules. High quality leads build confidence, through activity and property profiles as well as preliminary biological data, which might …

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In This Issue

Chiara Borsari

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