Synthesis, biological evaluation and molecular docking studies of some novel cyclopropane carbohydrazide derivatives as potential anticancer agents

Abstract

The synthesis of novel series of cyclopropane carbohydrazides is described viaKnoevenagel condensation of 2-furfuraldehyde with malonic acid in five steps. Condensation of the key intermediate 2-(furan-2-yl)cyclopropanecarbohydrazide (4)with heteroaryl/aryl aldehydes (a-t) in presence of ZnO NP in ethanol resulted in substituted N- hetero/arylidene-2-(furan-2-yl) cyclopropane carbohydrazides (5a-t). These compounds were screened for their anticancer activity against a panel of four cancer cell lines and four compounds showed promising activity at micromolar concentration against all the tested cell lines with IC50 values ranging between 1.9-8.45 μM. These compounds were further validated with in silico methods at the anticancer target, colchicine binding site. Synthesis of substituted N- hetero/arylidene-2-(furan-2-yl) cyclopropane carbohydrazides. These compounds were screened for their anticancer activity against a panel of four cancer cell lines and four compounds showed promising activity at micromolar concentration against all the tested cell lines with IC50 values ranging between 1.9-8.45 µM.