title: Synthesis and antitumor activity of 5,6-dihydro-17-hydroxy icogenin analogs.
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.
authors.affiliation: 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.
authors.forename: Yu-yao
authors.initials: YY
authors.lastname: Guan
authors.forename: Dan
authors.initials: D
authors.lastname: Zheng
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yan
authors.forename: Nan
authors.initials: N
authors.lastname: Wang
authors.forename: Ping-sheng
authors.initials: PS
authors.lastname: Lei
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D006801:Humans; D012503:Saponins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013256:Steroids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C574520:5,6-dihydro-17-hydroxy icogenin; D000970:Antineoplastic Agents; C496798:Icogenin; D012503:Saponins; D013256:Steroids