Morpholine hydrazone scaffold: Synthesis, anticancer activity and docking studies

来源 :Chinese Chemical Letters | 被引量 : 0次 | 上传用户:wlcbgtxx
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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 Hep G2(human hepatocellular liver carcinoma) and MCF-7(human breast adenocarcinoma). Analogs 13 had similar substantial cytotoxic effects towards Hep G2 with IC_(50) value 6.31±1.03μmmol/L when compared with the standard Doxorubicin(IC_(50)value 6.00±0.80μmmol/L); while compounds 5,8 and 9 showed potent cytotoxicity against MCF-7 with IC_(50) value 7.08±0.42μmmol/L, 1.26±0.34μmmol/L and11.22±0.22μmmol/L respectively when compared with the standard Tamoxifen(IC_(50)= 11.00±0.40μmol/L). Molecular docking studies also performed to understand the binding interaction. 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 Hep G2 (human hepatocellular liver carcinoma) and MCF-7 (human breast adenocarcinoma). Analogs 13 had similar cytotoxic effects toward Hep G2 with IC 50 value 6.31 ± 1.03 μmmol / L when compared with the standard Doxorubicin (IC 50 value 6.00 ± 0.80 μmmol / L); while compounds 5,8 and 9 showed potent cytotoxicity against MCF-7 with IC 50 value 7.08 ± 0.42 1.26 ± 0.34 μmmol / L and 11.22 ± 0.22 μmmol / L respectively when compared with the standard Tamoxifen (IC 50 = 11.00 ± 0.40 μιηοΙ / L). Molecular docking studies also performed to understand the binding interaction.
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