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
  • 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: [email protected].
  • 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: [email protected].
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.