Synthetic Modulation Including Structure Establishment, Antiproliferative Activity of Some p-Aryl Substituted (Z)-2-Cyanoethylideneacetohydrazides, and their Structure Activity Relationship

Abstract

A series of substituted aryl-2-cyanoethylideneacetohydrazides derivatives I [R = H, 4-MeO, 3-pyridyl, etc.] were successfully synthesized in the laboratory (yield 60-80%). The synthesized compounds I were screened for their antiproliferative activity against MCF-7 (estrogen dependent human breast cancer cell line), SaOS-2 (osteosarcoma cell line), and K562 (myeloid leukemia cell line) by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) reduction assay. They showed moderate to mild antiproliferative activity, compound I [R = NO2] being the most potent in the series with an IC50 55, 64 and 35 μM against MCF-7, SaOS-2 and K562 cell lines, depict nitro as a better antiproliferative substituent comparatively. 'Electron withdrawing phenomenon affects antiproliferative activity' -hypothesis was also tested.