Document Type

Article

Publication Date

11-1-2009

Publication Title

Steroids

Abstract

Hydroximinosteroids isolated from marine sponges display a variety of biological functions including cytotoxicity and anti-virus. In this study, we synthesized a series of hydroximinosteroid derivatives with a different functional group on the ring A or B and various side chains at position 17, and analyzed the cytotoxicity of these compounds against sk-Hep-1, H-292, PC-3 and Hey-1B cancer cells. Our results revealed that although a cholesterol-type side chain at position 17 is required for the biological activity of the compounds as we previously confirmed, elimination of the 4,5-double bond augmented the cytotoxic activity for the steroidal oximes. In addition, the presence of a hydroxy on 3- or 6-position of the steroidal nucleus resulted in a remarkable increase of cytotoxic activity. Our findings present more evidence showing the relationship between the chemical structure and biological function.

Comments

The authors acknowledge the financial support of the National Natural Science Foundation of China (no.: 20562001), the Natural Science Foundation of Guangxi Province (no.: 0832106) and the Foundation of Guangxi Education Bureau (200707M5172).

Creative Commons License

Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License.

DOI

10.1016/j.steroids.2009.07.009

Version

Postprint

Volume

74

Issue

12

Included in

Chemistry Commons

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