Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones. (15th April 2022)

• Record Type: Journal Article
• Authors: Chen, Chen; Luo, Yang; Yin, Honglu; Zhong, Qiu; Zheng, Shilong; Liu, Rui; Zhao, Chong; Wang, Guangdi; He, Ling
• Is Part Of: Bioorganic & medicinal chemistry. Volume 60(2022)
• Publication Date: 2022-04-15
• Subjects: Acyl sulfonamides spirodienone -- Anti-proliferation -- Apoptosis -- MMP2 inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2022.116626
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: 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.