2. Academic Validation
  3. Discovery of novel bis-evodiamine derivatives with potent antitumor activity

Discovery of novel bis-evodiamine derivatives with potent antitumor activity

  • Bioorg Med Chem. 2022 Jul 1;65:116793. doi: 10.1016/j.bmc.2022.116793.
Huixin Liang 1,  Wei Wang 2,  Fugui Zhu 1,  Shuqiang Chen 3,  Dan Liu 4,  Chunquan Sheng 5
Affiliations

Affiliations

  • 1 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, PR China; Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China.
  • 3 Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China. Electronic address: [email protected].
  • 4 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, PR China. Electronic address: [email protected].
  • 5 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, PR China; Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, PR China. Electronic address: [email protected].
PMID: 35550978 DOI: 10.1016/j.bmc.2022.116793
Abstract

Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell Apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.

Keywords

Antitumor activity; Apoptosis; Bis-evodiamine; Twin drug.

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