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Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2017-11-09 00:00:00 , DOI: 10.1021/acs.jmedchem.7b01388
Jose Antonio Ortega 1 , Laura Riccardi 1 , Elirosa Minniti 1, 2 , Marco Borgogno 1 , Jose M. Arencibia 1 , Maria L. Greco 3 , Anna Minarini 2 , Claudia Sissi 3 , Marco De Vivo 1, 4
Affiliation  

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.

中文翻译:

药理学杂交发现具有潜在的抗增殖活性的新型拓扑异构酶II毒药。

我们使用了药效团杂交策略,结合了Merbarone和依托泊苷的关键结构要素,并产生了新的II型拓扑异构酶(topoII)毒物。第一组杂合的topoII毒物对人类癌细胞显示出有希望的抗增殖活性,从而支持其进一步探索抗癌药物的发现。
更新日期:2017-11-09
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