학술논문
Design, Synthesis and Antitumor Activity of 1 H -indazole-3-amine Derivatives.
Document Type
Article
Source
Subject
*ANTINEOPLASTIC agents
*CHRONIC myeloid leukemia
*MOLECULAR hybridization
*CELL cycle
*CELL lines
*DASATINIB
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Language
ISSN
1661-6596
Abstract
A series of indazole derivatives were designed and synthesized by molecular hybridization strategy, and these compounds were evaluated the inhibitory activities against human cancer cell lines of lung (A549), chronic myeloid leukemia (K562), prostate (PC-3), and hepatoma (Hep-G2) by methyl thiazolyl tetrazolium (MTT) colorimetric assay. Among these, compound 6o exhibited a promising inhibitory effect against the K562 cell line with the IC50 (50% inhibition concentration) value of 5.15 µM, and this compound showed great selectivity for normal cell (HEK-293, IC50 = 33.2 µM). Moreover, compound 6o was confirmed to affect apoptosis and cell cycle possibly by inhibiting Bcl2 family members and the p53/MDM2 pathway in a concentration-dependent manner. Overall, this study indicates that compound 6o could be a promising scaffold to develop an effective and low-toxic anticancer agent. [ABSTRACT FROM AUTHOR]