Document Type

Article

Publication Date

2014

Publication Title

Marine Drugs

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.

Comments

The authors acknowledge the financial support of the Natural Science Foundation of Guangxi Province (No:2010GXNSFD013019), Natural Science Fund of Education Department of Guangxi province (No. 201202ZD059) and The Training Project for Excellent Middle-aged/Young Teachers in Guangxi Higher Education Institutions.

Creative Commons License

Creative Commons Attribution 4.0 License
This work is licensed under a Creative Commons Attribution 4.0 License.

DOI

10.3390/md12041715

Version

Publisher's PDF

Volume

12

Issue

4

Included in

Chemistry Commons

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