2. Academic Validation
  3. Synthesis and biological activity of salinomycin-hydroxamic acid conjugates

Synthesis and biological activity of salinomycin-hydroxamic acid conjugates

  • Bioorg Med Chem Lett. 2017 Apr 1;27(7):1624-1626. doi: 10.1016/j.bmcl.2017.01.080.
Bo Li 1,  Jun Wu 2,  Wenxuan Zhang 3,  Zhongwen Li 4,  Gang Chen 2,  Qi Zhou 2,  Song Wu 5
Affiliations

Affiliations

  • 1 State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China.
  • 2 State Key Laboratory of Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China.
  • 3 State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China. Electronic address: wxzhang@imm.ac.cn.
  • 4 University of Chinese Academy of Sciences, Beijing 100049, China.
  • 5 State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China. Electronic address: ws@imm.ac.cn.
PMID: 28262526 DOI: 10.1016/j.bmcl.2017.01.080
Abstract

Several salinomycin-hydroxamic acid conjugates were designed and synthesized. Most conjugates showed better antiproliferative activities than salinomycin in HT-29 colon Cancer, HGC-27 gastric Cancer, and especially in MDA-MB-231 triple-negative human breast Cancer cells. These conjugates are stable in Cell Culture media, and they showed much better biological activities than the 1:1 physical mixture with hydroxamic acids and salinomycin. The better membrane permeability and hydrolysis rate of the conjugates may lead to the activity improvements.

Keywords

Anti-cancer; Conjugates; Hydroxamic acid; Salinomycin.

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