Mar. Drugs 2014, 12(4), 1715-1731; doi:10.3390/md12041715
Synthesis and Evaluation of Some New Aza-B-homocholestane Derivatives as Anticancer Agents
1
Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China
2
School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China
3
Clinical Chemistry Program, Department of Chemistry, SI 424, Cleveland State University, Cleveland, OH 44115, USA
*
Author to whom correspondence should be addressed.
Received: 26 December 2013 / Revised: 24 February 2014 / Accepted: 26 February 2014 / Published: 25 March 2014
(This article belongs to the Special Issue Bioactivity-Focused Syntheses of Marine Natural Products and Congeners)
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.Keywords:
aza-B-homo-cholestane derivatives; anticancer agents; cytotoxicity; 3D multicellular spheroids screening; apoptosis
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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MDPI and ACS Style
Huang, Y.; Cui, J.; Chen, S.; Lin, Q.; Song, H.; Gan, C.; Su, B.; Zhou, A. Synthesis and Evaluation of Some New Aza-B-homocholestane Derivatives as Anticancer Agents. Mar. Drugs 2014, 12, 1715-1731.
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