title: Synthesis and evaluation of some new aza-B-homocholestane derivatives as anticancer agents.
abstract: Using analogues of some marine steroidal oximes as precursors, a series of aza-B-homocholestane derivatives possessing different substituted groups at the 3-position of the steroidal nucleus were synthesized. Their biological activity against cancer cell proliferation was determined with multiple cancer cell lines. Aza-B-homocholestane derivatives possessing 3-hydroxyl, 3-hydroximino and 3-thiosemicarbazone groups displayed remarkable cytotoxicity to cancer cells via apoptosis inducing mechanism. Compounds 5, 10, 12, 15 and 18 exhibited better potency to inhibit cancer cell proliferation. In addition, compound 15 was further evaluated with three dimensional (3D) multicellular spheroids assay to determine its potency against spheroid growth. The structure-activity relationship (SAR) generated in the studies is valuable for the design of novel chemotherapeutic agents.
authors.affiliation: Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China. huangyanmin828@163.com.
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Huang
authors.affiliation: Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China. cuijg1954@126.com.
authors.forename: Jianguo
authors.initials: J
authors.lastname: Cui
authors.affiliation: Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China. huaxue37z@126.com.
authors.forename: Sijing
authors.initials: S
authors.lastname: Chen
authors.affiliation: Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China. linqifu335@163.com.
authors.forename: Qifu
authors.initials: Q
authors.lastname: Lin
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China. YjhXhc@mail.sysu.edu.cn.
authors.forename: Huacan
authors.initials: H
authors.lastname: Song
authors.affiliation: Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China. ganchunfang2008@126.com.
authors.forename: Chunfang
authors.initials: C
authors.lastname: Gan
authors.affiliation: Clinical Chemistry Program, Department of Chemistry, SI 424, Cleveland State University, Cleveland, OH 44115, USA. b.su@csuohio.edu.
authors.forename: Bin
authors.initials: B
authors.lastname: Su
authors.affiliation: Clinical Chemistry Program, Department of Chemistry, SI 424, Cleveland State University, Cleveland, OH 44115, USA. a.zhou@csuohio.edu.
authors.forename: Aimin
authors.initials: A
authors.lastname: Zhou
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002776:Cholestanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013256:Steroids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002776:Cholestanes; D013256:Steroids