Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and Anticancer Activity

Title: Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and Anticancer Activity

Volume: 9 Issue: 2

Author(s): Xian-Hai Lv, Xiu-Li Zhang, Xin-Hua Liu and Lei Shi

Affiliation:

Keywords: Coumarins, Dihydropyrazole, Molecular Docking, Anticancer activity, Telomerase, chromosomal integrity, 3DU6, gastric SGC-7901, dihydropyrazole heterocycle, Claisen-Schmidt, mother liquor, column chromatography, Cytotoxic Assay, Colorless crystals

Abstract: Seven novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substituted-phenyl-4,5-dihydro-1Hpyrazol- 3-yl)-2H-chromen-2-one derivatives were synthesized and characterized by 1H NMR and 13 C NMR. All of the compounds have been screened for their anticancer activity. The bioassay tests show that compound 4g exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 6.99±1.10 μg/mL. Docking simulation was performed to position compound 4g into the telomerase (3DU6) active site to determine the probable binding model.

Cite this article as:

Lv Xian-Hai, Zhang Xiu-Li, Liu Xin-Hua and Shi Lei, Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and Anticancer Activity, Letters in Drug Design & Discovery 2012; 9 (2) . https://dx.doi.org/10.2174/157018012799079743

DOI https://dx.doi.org/10.2174/157018012799079743	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X