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An efficient and green one-pot four-component strategy for the synthesis of β-keto phosphorodithioates via difunctionalization of alkenes using air as the oxygen source and cheap phosphorus pentasulfide (PS) as the sulfur and phosphorus source has been successfully reported at room temperature. This method features simple operation, mild conditions, step economy, wide range of substrates, and the avoidance of moisture-sensitive reagents/pre-functionalized substrates. These advantages of this electrochemical protocol are consistent with the concept of green synthetic chemistry, providing a straightforward and efficient pathway to synthesize β-keto phosphorodithioate derivatives.
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http://dx.doi.org/10.1021/acs.orglett.5c01911 | DOI Listing |
J Med Chem
September 2025
State Key Laboratory of Bioactive Molecules and Druggability Assessment, Guangdong Basic Research Center of Excellence for Natural Bioactive Molecules and Discovery of Innovative Drugs, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery o
Aberrant activation of fibroblast growth factor receptors (FGFRs) plays a critical role in tumorigenesis across multiple cancer types, driving the development of various FGFR inhibitors. Despite clinical advances, therapeutic efficacy remains limited by the emergence of drug resistance, primarily mediated by gatekeeper mutations in FGFRs. To overcome this challenge, we designed and synthesized a novel series of 7-(1-methyl-1-indole-3-yl)-5-pyrrolo[2,3-]pyrazine derivatives as covalent pan-FGFR inhibitors targeting both wild-type and gatekeeper mutants.
View Article and Find Full Text PDFJ Med Chem
September 2025
Faculty of Mathematics and Natural Sciences, Institute of Pharmaceutical and Medicinal Chemistry, Heinrich Heine University Düsseldorf, 40225 Düsseldorf, Germany.
New treatment strategies are required to combat the spread of drug-resistant malaria. The synthesis and preclinical evaluation of novel 3-hydroxy-propanamidines (HPAs), with modifications of the phenanthrene and the 4-fluorobenzamidine moieties, has yielded several analogs exhibiting excellent in vitro growth inhibition of drug-sensitive or resistant fresh clinical isolates and culture-adapted strains. No cytotoxicity in the human HepG2 cell line was observed, demonstrating notable parasite selectivity.
View Article and Find Full Text PDFJMIR Med Inform
September 2025
Department of Hepatobiliary and Vascular Surgery, First Affiliated Hospital of Chengdu Medical College, Chengdu, China.
Background: Primary liver cancer, particularly hepatocellular carcinoma (HCC), poses significant clinical challenges due to late-stage diagnosis, tumor heterogeneity, and rapidly evolving therapeutic strategies. While systematic reviews and meta-analyses are essential for updating clinical guidelines, their labor-intensive nature limits timely evidence synthesis.
Objective: This study proposes an automated literature screening workflow powered by large language models (LLMs) to accelerate evidence synthesis for HCC treatment guidelines.
JMIR Hum Factors
September 2025
College of Biomedical Engineering & Instrument Science, Zhejiang University, Hangzhou, China.
Background: The rapid advancement of next-generation sequencing has significantly expanded the landscape of precision medicine. However, health care professionals face increasing challenges in keeping pace with the growing body of oncological knowledge and integrating it effectively into clinical workflows. Precision oncology decision support (PODS) tools aim to assist clinicians in navigating this complexity, yet their current functionalities only partially address clinical needs.
View Article and Find Full Text PDFOrg Lett
September 2025
Frontiers Science Center for Transformative Molecules, State Key Laboratory of Polyolefins and Catalysis, State Key Laboratory of Synergistic Chem-Bio Synthesis, Zhang Jiang Institute for Advanced Study, Shanghai Jiao Tong University, Shanghai 200240, China.
C-labeled α-amino acids are important molecules in biological studies and drug development. Cost-effective synthesis of α-amino acids with a high level of C incorporation under mild conditions remains limited. Herein, we report the development of a benzylic C(sp)-H carboxylation method to prepare highly C-labeled α-amino acids, i.
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