title: Synthesis and cytotoxic activity of some 4,6-diaza-A,B-dihomo-steroid bilactams.
abstract: Using cholesterol, stigmasterol and sitosterol as starting materials, some 4,6-diaza-A,B-dihomo-steroid bilactams were synthesized via two different synthetic routes by oxidation, reduction, oximation, Beckman rearrangement, etc. The cytotoxic activity of the synthesized compounds against SGC 7901 (human ventriculi carcinoma), Bel-7404 (human liver carcinoma), HeLa (human cervical carcinoma) and HT-29 (colonic carcinoma) cancer cells were investigated. The results showed that compounds 2 and 7b displayed a good cytotoxic activity to the SGC 7901, Bel 7404 and HeLa tumor cell lines with the IC50 values of 11.6, 16.4, 13.9 and 13.1, 21.8, 13.1 μmol/L, respectively. Their cytotoxic activity is almost same as cisplatin to these cells. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs.
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
authors.forename: Jianguo
authors.initials: J
authors.lastname: Cui
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
authors.forename: Qifu
authors.initials: Q
authors.lastname: Lin
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
authors.forename: Chunfang
authors.initials: C
authors.lastname: Gan
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
authors.forename: Qiucui
authors.initials: Q
authors.lastname: Yao
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Su
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China. Electronic address: huangyanmin828@163.com.
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Huang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001378:Azasteroids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002784:Cholesterol / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells; D006367:HeLa Cells; D006718:Homosteroids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007769:Lactams; D008956:Models, Chemical; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D012855:Sitosterols / Q000737:chemistry; D013256:Steroids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013265:Stigmasterol / Q000737:chemistry
chemical_list: C000590999:4,6-diaza-A,B-dihomo-24-ethylcholest-3,7-dione; C000591000:4,6-diaza-A,B-dihomocholest-3,7-dione; D000970:Antineoplastic Agents; D001378:Azasteroids; D006718:Homosteroids; D007769:Lactams; D012855:Sitosterols; D013256:Steroids; C025473:gamma-sitosterol; D002784:Cholesterol; D013265:Stigmasterol
keywords: 4,6-Diaza-A,B-dihomo-steroid bilactams; Cholesterol; Cytotoxicity; Sitosterol; Stigmasterol