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 ...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.展开更多
基金financial support under theFundamental Research Grant Scheme(FRGS)with sponsorship reference numbers FRGS/1/2015/SG05/Ui TM/02/6financial support under the reference number 600-RMI/FRGS5/3(135/2015)
文摘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.
