基于药效团杂交发现具有潜在抗增殖活性的新型拓扑异构酶 II 抑制剂。
Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity.
机构信息
Laboratory of Molecular Modeling and Drug Discovery, Istituto Italiano di Tecnologia , Via Morego 30, 16163 Genova, Italy.
Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna , Via Belmeloro 6, 40126 Bologna, Italy.
出版信息
J Med Chem. 2018 Feb 8;61(3):1375-1379. doi: 10.1021/acs.jmedchem.7b01388. Epub 2017 Nov 9.
We used a pharmacophore hybridization strategy to combine key structural elements of merbarone and etoposide and generated new type II topoisomerase (topoII) poisons. This first set of hybrid topoII poisons shows promising antiproliferative activity on human cancer cells, endorsing their further exploration for anticancer drug discovery.
我们采用药效团杂交策略，将美迪诺酮和依托泊苷的关键结构要素结合起来，生成了新型的拓扑异构酶 II（topoII）抑制剂。这第一组杂交型 topoII 抑制剂对人类癌细胞表现出有前景的抗增殖活性，支持进一步探索其作为抗癌药物的发现。
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