Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives containing benzodioxole as potential anticancer agents

HH Wang, KM Qiu, HE Cui, YS Yang, M Xing…

Index: Wang, Hai-Hong; Qiu, Ke-Ming; Cui, Hong-En; Yang, Yu-Shun; Yin-Luo; Xing, Man; Qiu, Xiao-Yang; Bai, Li-Fei; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 2 p. 448 - 455

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Citation Number: 19

Abstract

A series of novel thiazolyl-pyrazoline derivatives containing benzodioxole (C1–C20) have been designed and synthesized. Among of the synthesized compounds, 2-(5-(benzo [d][1, 3] dioxol-5-yl)-3-(4-bromophenyl)-4, 5-dihydro-1H-pyrazol-1-yl)-4-(4-bromophenyl) thiazole (C6) displayed the most potent inhibitory activity for HER-2 (IC50= 0.18 μM for HER-2). Antiproliferative assay results indicated that compound C6 owned high antiproliferative ...