| Summary: | 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 μmol/L when compared with the standard Doxorubicin (IC50 value 6.00 ± 0.80 μmol/L); while compounds 5, 8 and 9 showed potent cytotoxicity against MCF-7 with IC50 value 7.08 ± 0.42 μmol/L, 1.26 ± 0.34 μmol/L and 11.22 ± 0.22 μmol/L respectively when compared with the standard Tamoxifen (IC50 = 11.00 ± 0.40 μmol/L). Molecular docking studies also performed to understand the binding interaction. © 2016 Muhammad Taha, Syed Adnan Ali Shah
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