Microwave-assisted single-step synthesis of cyclic and acyclic β-aminosulfones and evaluation of their antifungal activity targeting CYP51 [0.03%]
一步合成环状和非环状β-氨基磺胺衍生物及其抗真菌活性评价
Abigail Bibiana Pinheiro,Soumik Saha,Madhuri Madduri et al.
Abigail Bibiana Pinheiro et al.
The alarming rise of drug resistance has created an urgent need for novel antifungal agents. On the other hand, growing environmental concerns necessitate the development of sustainable alternatives to conventional synthetic methods for act...
Novel pyrimido[1,2- a]imidazole derivatives as potent Pks13-TE inhibitors: structure-based virtual screening and rational design [0.03%]
基于结构的虚拟筛选和合理设计新的Pks13-TE强效抑制剂嘧啶并[1,2-a]咪唑衍生物
Xiangying Li,Yuanyuan Liu,Wen Shao et al.
Xiangying Li et al.
Tuberculosis (TB) remains a major global health threat, exacerbated by the emergence of drug-resistant strains. The mycobacterial enzyme Pks13 has emerged as a promising drug target for novel anti-TB agents. We herein report the design, syn...
The many facets of sustainability in medicinal chemistry: our personal experience [0.03%]
药物化学各方面的可持续性：个人经验
Bianca Martinengo,Eleonora Diamanti,Elisa Uliassi et al.
Bianca Martinengo et al.
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 Health into drug design and development may d...
Editorial
RSC medicinal chemistry. 2025 Dec 30. DOI:10.1039/d5md00882d 2025
A new compound that extends the lifespan of worms, with favorable in vitro properties and a lack of toxicity in rodents [0.03%]
一种新的化合物可延长线虫寿命具有良好的体外特性且对啮齿类动物无毒
Heidi M Blank,Michael Polymenis
Heidi M Blank
The development of geroprotectors, compounds that slow the biological aging process, is an important goal in modern medicine. These interventions hold the promise not only of extending lifespan, but more importantly, of extending healthspan...
N-Cyano sulfoximine-mediated thiazole ligation with N-terminal cysteine under mild aqueous conditions [0.03%]
温和水相条件下天冬酰胺-N-氰基硫氧甲酰亚胺介导的含巯基氨基酸与噻唑
Eunsil Kim,Ji Young Hyun,Ji Ho Song et al.
Eunsil Kim et al.
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 selectivity, tunable reactivity, and improved d...
On the history, synthesis, and medicinal use of cantharidin, LB-100, and their analogs [0.03%]
关于斑蝥素、LB-100及其类似物的历史、合成和药用的综述
Kevin A Scott,Adam McCluskey,Jon T Njardarson et al.
Kevin A Scott et al.
Cantharidin, a defensive toxin produced by blister beetles, has fascinated chemists, physicians, and historians for centuries. From its notorious use as the aphrodisiac "Spanish fly" to its modern FDA approval as YCANTH™ for molluscum cont...
Crystallographic characterisation and development of bi-substrate inhibitors of coronavirus nsp14 methyltransferase [0.03%]
冠状病毒nsp14甲基转移酶的双底物抑制剂的晶体学表征及研发
Irene Georgiou,Colin Robinson,Sean N O&#x;Byrne et al.
Irene Georgiou et al.
SARS-CoV-2 non-structural protein 14 (nsp14) is essential for viral mRNA cap guanine-N7 methylation and represents a promising but underexplored antiviral target. Herein we describe a structure-guided campaign based on a hit from a focussed...
Discovery of enaminone-linked benzofuran derivatives as dual VEGFR-2/hCA IX inhibitors exhibiting hypoxia-mediated chemosensitization [0.03%]
发现一类新型烯胺酮连接的苯并呋喃类化合物作为VEGFR-2/hCA IX双靶点抑制剂并能协同抗缺氧化疗
Wagdy M Eldehna,Zainab M Elsayed,Mohamed R Elnagar et al.
Wagdy M Eldehna et al.
The overexpression of VEGFR-2 and carbonic anhydrase IX (hCA IX), two proven therapeutic targets in aggressive malignancies, is closely associated with hypoxia-driven tumor growth. A novel series of enaminone-linked benzofuran compounds was...
Dual COX-2 and EGFR inhibition by pyrazole- ar-turmerone hybrids suppresses colorectal cancer cell proliferation [0.03%]
新型吡唑类双靶向COX-2和EGFR的体外抗结直肠癌活性研究
Monsin Sangsawat,Nonthaneth Nalinratana,Waraluck Chaichompoo et al.
Monsin Sangsawat et al.
Colorectal cancer (CRC) progression involves a coordinated interaction between COX-2-mediated inflammation and EGFR-driven proliferation. Current monotherapies often fail due to incomplete pathway suppression and resistance development, hig...
Unlocking the therapeutic potential of HDAC8-degrading PROTACs: progress, challenges, and future directions [0.03%]
HDAC8降解PROTACs的治疗潜力：进展、挑战与未来方向
Suvankar Banerjee,Nilanjan Adhikari,Balaram Ghosh
Suvankar Banerjee
Histone deacetylase 8 (HDAC8) is a class I enzyme associated with various diseases, including cancer and neurological disorders. Although small-molecule HDAC inhibitors have been developed, their lack of selectivity often leads to off-targe...