Antiproliferative Activity of Novel Derivative of Thiopyran on Breast and Colon Cancer Lines and DNA Binding
- 1 January 2012
- journal article
- research article
- Published by Mary Ann Liebert Inc in DNA and Cell Biology
- Vol. 31 (1), 128-134
- https://doi.org/10.1089/dna.2011.1291
Abstract
Dimethyl-5-acetyl-4-methyl-6-(4-methylphenylimino)-6H-thiopyran-2,3-dicarboxylate (4) has been synthesized and its antiproliferative activity is reported here. Compound 4 inhibited the growth of human colon cancer cell line HCT-15 with an IC50 value of 3.5 μM and of breast cancer cell line MCF-7 with an IC50 value of 1.5 μM in a dose/time-dependent manner using a sulforhodamine B assay. Moreover, suppression of clonogenic activity occurred after exposure to 4 at a concentration of 4 μM for HCT-15 and 1.7 μM for MCF-7. The results also showed tumor cell invasion through matrigel and cell adhesion. The effect of ligand complexation on DNA structure led to overall affinity constant of K4-DNA=9.8×104 M−1.This publication has 33 references indexed in Scilit:
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