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  3. Design, synthesis and QSAR study of novel isatin analogues inspired Michael acceptor as potential anticancer compounds

Design, synthesis and QSAR study of novel isatin analogues inspired Michael acceptor as potential anticancer compounds

  • Eur J Med Chem. 2018 Jan 20:144:493-503. doi: 10.1016/j.ejmech.2017.12.043.
Jiabing Wang 1,  Di Yun 1,  Jiali Yao 2,  Weitao Fu 3,  Fangyan Huang 2,  Liping Chen 2,  Tao Wei 2,  Cuijuan Yu 1,  Haineng Xu 1,  Xiaoou Zhou 1,  Yanqing Huang 2,  Jianzhang Wu 4,  Peihong Qiu 5,  Wulan Li 6
Affiliations

Affiliations

  • 1 Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China; Wenzhou Biomedical Innovation Center, Wenzhou University and Wenzhou Medical University, Wenzhou, Zhejiang 325035, China.
  • 2 Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China.
  • 3 Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China; College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China.
  • 4 Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China; Wenzhou Biomedical Innovation Center, Wenzhou University and Wenzhou Medical University, Wenzhou, Zhejiang 325035, China. Electronic address: wjzwzmu@163.com.
  • 5 Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China. Electronic address: wjzwzmc@126.com.
  • 6 Chemical Biology Research Center, College of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China; Wenzhou Biomedical Innovation Center, Wenzhou University and Wenzhou Medical University, Wenzhou, Zhejiang 325035, China; College of Information Science and Computer Engineering, The First Clinical Medical College, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China. Electronic address: lwlwzmu@163.com.
PMID: 29288946 DOI: 10.1016/j.ejmech.2017.12.043
Abstract

Molecular hybridization is considered as an effective tactic to develop drugs for the treatment of Cancer. A series of novel hybrid compounds of isatin and Michael acceptor were designed and synthesized on the basis of association principle. These hybrid compounds were tested for cytotoxic potential against human Cancer cell lines namely, BGC-823, SGC-7901 and NCI-H460 by MTT assay. Most compounds showed good anti-growth activities in all tested human Cancer cells. SAR and QSAR analysis may provide vital information for the future development of novel anti-cancer inhibitors. Notably, compound 6a showed potent growth inhibition on BGC-823, SGC-7901 and NCI-H460 with the IC50 values of 3.6 ± 0.6, 5.7 ± 1.2, 3.2 ± 0.7 μM, respectively. Besides, colony formation assays, wound healing assays and flow cytometry analysis indicated 6a exhibited a potent anti-growth and anti-migration ability in a concentration-dependence manner through arrested cells in the G2/M phase of cell cycle. Moreover, 6a significantly repressed tumor growth in a NCI-H460 xenograft mouse model. Overall, our findings suggested isatin analogues inspired Michael acceptor may provide promising lead compounds for the development of Cancer chemotherapeutics.

Keywords

Anticancer; Association principle; Chemotherapeutics; Quantitative structure-activity relationship.

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