Synthesis and antitumor activity of cholest-4 alpha-methyl-7-en-3beta-ol derivatives |
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Authors: | He Lan Liu Yumei Shi Jiangong Pei Qiang |
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Affiliation: | Department of Chemistry, Beijing Normal University, Beijing 100875, PR China. helan1961@yahoo.com.cn |
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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. |
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Keywords: | Cholest-4α-methyl-7-en-3β-ol Structural modification Antitumor activity |
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