Morpholine hydrazone scaffold: Synthesis, anticancer activity and docking studies

In this paper, synthesis and anticancer activities of morpholine hydrazones scaffold (1-17) thoroughly studied. Small series of morpholine hydrazones synthesized by treating 5-morpholinothiophene-2-carbaldehyde with different aryl hydrazides to form morpholine hydrazones scaffold (1-17). The in vitro anticancer potential of all these compounds was checked against human cancer cell lines like HepG2 (human hepatocellular liver carcinoma) and MCF-7 (human breast adenocarcinoma). Analogs 13 had similar substantial cytotoxic effects towards HepG2 with IC50 value 6.31 +/- 1.03 mu mol/L when compared with the standard Doxorubicin (IC50 value 6.00 +/- 0.80 mu mol/L); while compounds 5,8 and 9 showed potent cytotoxicity against MCF-7 with IC50 value 7.08 +/- 0.42 mu mol/L, 1.26 +/- 0.34 mu mol/L and 11.22 +/- 0.22 mu mol/L respectively when compared with the standard Tamoxifen (IC50 = 11.00 +/- 0.40 mu mol/L). Molecular docking studies also performed to understand the binding interaction. (C) 2016 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.