2. Academic Validation
  3. Synthesis and antitumor activity of 5,6-dihydro-17-hydroxy icogenin analogs

Synthesis and antitumor activity of 5,6-dihydro-17-hydroxy icogenin analogs

  • Eur J Med Chem. 2012 May:51:200-5. doi: 10.1016/j.ejmech.2012.02.043.
Yu-yao Guan 1,  Dan Zheng,  Zheng Yan,  Nan Wang,  Ping-sheng Lei
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, PR China.
PMID: 22429911 DOI: 10.1016/j.ejmech.2012.02.043
Abstract

Four 5,6-dihydro-17-hydroxy icogenin analogs were designed and synthesized. Their in vitro antitumor activities were tested by the standard MTT assay. Compound 22 (IC(50) = 3.38-8.30 μM) and compound 23 (IC(50) = 1.90-9.69 μM) showed potential antitumor activities against the entire tested seven Cancer cell lines. The SAR (structure activity relationship) research showed that the introduction of 17-hydroxy lowered the antitumor activity to an extent.

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