2. Academic Validation
  3. Synthesis and biological evaluation of heteroaryl styryl sulfone derivatives as anticancer agents

Synthesis and biological evaluation of heteroaryl styryl sulfone derivatives as anticancer agents

  • Bioorg Med Chem Lett. 2016 Dec 1;26(23):5674-5678. doi: 10.1016/j.bmcl.2016.10.062.
Yi Long 1,  Mingfeng Yu 1,  Peng Li 1,  Saiful Islam 1,  Aik Wye Goh 1,  Malika Kumarasiri 1,  Shudong Wang 2
Affiliations

Affiliations

  • 1 Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5001, Australia.
  • 2 Centre for Drug Discovery and Development, Sansom Institute for Health Research and School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5001, Australia. Electronic address: shudong.wang@unisa.edu.au.
PMID: 27815119 DOI: 10.1016/j.bmcl.2016.10.062
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 compound 14f 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 that 14f caused cell-cycle arrest at the G2/M phase and induced Apoptosis by targeting CDC25C and Mcl-1 proteins in A2780 ovarian cells.

Keywords

Anti-cancer agents; Kinase inhibitor; Non-ATP competitive inhibition; Polo-like kinase 1; Ras-driven signaling pathways.

Figures