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Design, Synthesis and Antitumor Activity of 1H-indazole-3-amine Derivatives.

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.

SUBMITTER: Wang C

PROVIDER: S-EPMC10218234 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature

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Design, Synthesis and Antitumor Activity of 1H-indazole-3-amine Derivatives.

Wang Congyu C Zhu Mei M Long Xuesha X Wang Qin Q Wang Zhenchao Z Ouyang Guiping G

International journal of molecular sciences 20230512 10

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 ...[more]

PMID: 37240028

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