Literature

Abstract

The synthesis and biological evaluation of a new library of 4-(1,2-diarylbut-1-en-1-yl)isobutyranilides is described. The new compounds were found to be cytotoxic in the micromolar range in two human tumor cell lines, MCF-7 (mammary gland adenocarcinoma) and HeLa (cervix adenocarcinoma) and two human ovarian cancer cell lines (A2780 and OVCAR5). Detailed studies on the most active compound 6g show that it was able to induce apoptosis and suggest topoisomerase II as a possible intracellular target. The relevance of the interaction of the most active compound with topoisomerase II is demonstrated and supported by docking studies.

DOI： 10.1016/j.ejmech.2016.03.090

4-(1,2-diarylbut-1-en-1-yl)isobutyranilide derivatives as inhibitors of topoisomerase II

European Journal of Medicinal Chemistry 2016.0

Design and synthesis of novel 2,4-diaryl-5H-indeno[1,2-b]pyridine derivatives, and their evaluation of topoisomerase inhibitory activity and cytotoxicity

Bioorganic & Medicinal Chemistry 2015.0

One pot synthesis, in silico study and evaluation of some novel flavonoids as potent topoisomerase II inhibitors

Bioorganic & Medicinal Chemistry Letters 2021.0

2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure–activity relationship, and docking study

Bioorganic & Medicinal Chemistry Letters 2010.0

Synthesis and biological evaluation of N -(carbobenzyloxy)- l -phenylalanine and N -(carbobenzyloxy)- l -aspartic acid- β -benzyl ester derivatives as potent topoisomerase IIα inhibitors

Bioorganic & Medicinal Chemistry 2017.0

Synthesis of rotenoid derivatives with cytotoxic and topoisomerase II inhibitory activities