E-pharmacophore guided discovery of pyrazolo[1,5-c]quinazolines as dual inhibitors of topoisomerase-I and histone deacetylase.

Gaurav Joshi,Sourav Kalra,Umesh Prasad Yadav,Praveen Sharma,Pankaj Kumar Singh,Suyog Amrutkar,Arshad J Ansari,Santosh Kumar,Ashoke Sharon,Sadhana Sharma,Devesh M Sawant,Uttam C Banerjee,Sandeep Singh,Raj Kumar

Bioorganic Chemistry（2020）

引用 22|浏览11

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摘要

•Non-camptothecin analogues among 11 motifs of pyrazoloquinazolines are reported.•E-pharmacophore drug design guided discovery of Topoisomerase I inhibitors.•Topoisomerase I inhibitors induced apoptosis and were non-DNA intercalators.•4a emerged as a dual inhibitor of Topoisomerase I-HDAC1 with potentiated anticancer effect.

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关键词

E-pharmacophore,Pyrazolo[1,5-c]quinazolines,Topoisomerase inhibitors,Histone deacetylases,Dual inhibitors,3D Culture

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