Synthesis and antitumor activity of cholest-4 alpha-methyl-7-en-3beta-ol derivatives.

Abstract

Cholest-4 alpha-methyl-7-en-3beta-ol (1) has potent inhibitory activity against pc 12 tumor with 0.5043 ratio (10 microg/mL). This paper describes a series of structural modification of this compound, which focus on 3beta-hydroxyl group and 7(8)-double bond. The synthesized derivatives of 1 were tested for human cancer cell lines including colon cancer (HCT-8), liver cancer (BEL-7402) and nasopharyngeal cancer (KB) cells. The results showed that cholest-4 alpha-methyl-8-en-3beta,7 alpha-diol 6a inhibits KB cell significantly with IC(50) 1.32 x 10(-9)microg/mL. In addition, the cytotoxic properties of this compound against HCT-8 and BEL-7402 are excellent with IC(50) 1.2 microg/mL.

• Authors: Lan He, Yumei Liu, Jiangong Shi, Qiang Pei
• Journal: Steroids (Steroids) Vol. 71 Issue 6 Pg. 476-83 (Jun 2006) ISSN: 0039-128X [Print] United States
• PMID: 16504229 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antineoplastic Agents
• Esters
• Plant Extracts
• Cholesterol

Topics

• Antineoplastic Agents (pharmacology)
• Cell Line, Tumor
• Cholesterol (analogs & derivatives, chemical synthesis, chemistry, metabolism, pharmacology)
• Dracaena (chemistry)
• Esters
• HeLa Cells
• Humans
• In Vitro Techniques
• Inhibitory Concentration 50
• Isomerism
• Plant Extracts (chemistry)
• Structure-Activity Relationship