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Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.

ABSTRACT: Based on the promising results of benzenesulfonamide spirodienones as antineoplastic agents, we have designed and synthesized a series of novel acyl sulfonamides spirodienone for antineoplastic evaluation. Of these, compound 4a exhibited remarkable in vitro antiproliferative activity by arresting the cell cycle and inducing apoptosis of MDA-MB-231 cells. Acute toxicity study has demonstrated 4a at 100 mg/kg dose caused no obvious toxicity to the major organs of mice. Moreover, compound 4a suppressed the growth of murine 4T1 tumor in vivo. Preliminary enzyme assay showed that 4a was a potential MMP2 inhibitor for cancer therapy. In all, these results indicate that compound 4a may be a lead compound for the development of anticancer agents.

SUBMITTER: Chen C

PROVIDER: S-EPMC9675047 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature

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Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.

Chen Chen C Luo Yang Y Yin Honglu H Zhong Qiu Q Zheng Shilong S Liu Rui R Zhao Chong C Wang Guangdi G He Ling L

Bioorganic & medicinal chemistry 20220111

Based on the promising results of benzenesulfonamide spirodienones as antineoplastic agents, we have designed and synthesized a series of novel acyl sulfonamides spirodienone for antineoplastic evaluation. Of these, compound 4a exhibited remarkable in vitro antiproliferative activity by arresting the cell cycle and inducing apoptosis of MDA-MB-231 cells. Acute toxicity study has demonstrated 4a at 100 mg/kg dose caused no obvious toxicity to the major organs of mice. Moreover, compound 4a suppre ...[more]

PMID: 35255412

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