Synthesis and antitumor activity of cholest-4 alpha-methyl-7-en-3beta-ol derivatives.
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.
He
Lan
L
Department of Chemistry, Beijing Normal University, Beijing 100875, PR China. helan1961@yahoo.com.cn
Liu
Yumei
Y
Shi
Jiangong
J
Pei
Qiang
Q
D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002784:Cholesterol / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D031409:Dracaena / Q000737:chemistry; D004952:Esters; D006367:HeLa Cells; D006801:Humans; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D007536:Isomerism; D010936:Plant Extracts / Q000737:chemistry; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004952:Esters; D010936:Plant Extracts; D002784:Cholesterol