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.
This is an open access article distributed under the
Creative Commons Attribution License which permits unrestricted use, distribution,
and reproduction in any medium, provided the original work is properly cited.
Export to
BibTeX |
EndNote
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.
AMA 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. Marine Drugs. 2014; 12(4):1715-1731.
Chicago/Turabian Style
Huang, Yanmin; Cui, Jianguo; Chen, Sijing; Lin, Qifu; Song, Huacan; Gan, Chunfang; Su, Bin; Zhou, Aimin. 2014. "Synthesis and Evaluation of Some New Aza-B-homocholestane Derivatives as Anticancer Agents." Mar. Drugs 12, no. 4: 1715-1731.
Twitter
Facebook
Mendeley
CiteULike
