Synthesis and Evaluation of Some New Aza-B-homocholestane Derivatives as Anticancer Agents

Marine Drugs

Yanmin Huang³  Jianguo Cui³  Sijing Chen³  Qifu Lin³  Huacan Song¹  Chunfang Gan³  Bin Su² 

[1] School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China; E-Mail:;Clinical Chemistry Program, Department of Chemistry, SI 424, Cleveland State University, Cleveland, OH 44115, USA; E-Mails:;Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China; E-Mails:

关键词: aza-B-homo-cholestane derivatives;    anticancer agents;    cytotoxicity;    3D multicellular spheroids screening;    apoptosis;   

DOI  :  10.3390/md12041715

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.