Synthesis and biological evaluation of heteroaryl styryl sulfone derivatives as anticancer agents. Issue 23 (1st December 2016)

• Record Type: Journal Article
• Authors: Long, Yi; Yu, Mingfeng; Li, Peng; Islam, Saiful; Goh, Aik Wye; Kumarasiri, Malika; Wang, Shudong
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 23(2016)
• Page Start: 5674
• Page End: 5678
• Publication Date: 2016-12-01
• Subjects: Kinase inhibitor -- Polo-like kinase 1 -- Ras-driven signaling pathways -- Non-ATP competitive inhibition -- Anti-cancer agents; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.10.062
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Herein we disclose a series of novel heteroaryl styryl sulfone derivatives as potential anticancer agents. Structure-activity relationships of these newly synthesised compounds were explored with respect to the significance of the position and number of nitrogen atom of the heteroaryl ring for anti-proliferative activity in human cancer cell lines. A lead compound14f was tested against a panel of cancerous and untransformed cell lines, and found to be highly potent against cancer cells with minimal toxicity in the untransformed cells. Further mechanistic studies uncovered that14f caused cell-cycle arrest at the G2/M phase and induced apoptosis by targeting CDC25C and Mcl-1 proteins in A2780 ovarian cells.