title: Synthesis and cytotoxicity of 17a-aza-D-homo-androster-17-one derivatives.
abstract: A series of 17a-aza-D-homo-andrester-17-one derivatives, bearing hydroxyl, hydroximino, carbonyl and thiosemicarbazido groups at the position-3 or position-6 of steroidal nucleus, were prepared and evaluated in vitro against two human cell lines (Hela (human cervical carcinoma) and SMMC 7404 (human liver carcinoma)). The results showed that these compounds could exhibit a high cytotoxicity to Hela tumor cell line, especially for compounds 8 and 12, the IC(50) values are 15.1 and 14.0 nmol/mL, respectively. Our findings could provide new evidence showing the relationship between the chemical structure and biological activity and may be useful for the discovery of new anti-cancer drugs.
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou, PR China.
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Huang
authors.forename: Jianguo
authors.initials: J
authors.lastname: Cui
authors.forename: Zhengguo
authors.initials: Z
authors.lastname: Zhong
authors.forename: Chunfang
authors.initials: C
authors.lastname: Gan
authors.forename: Wenyan
authors.initials: W
authors.lastname: Zhang
authors.forename: Huacan
authors.initials: H
authors.lastname: Song
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D013256:Steroids / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D013256:Steroids