Synthesis and antitumor activity of cholest-4α-methyl-7-en-3β-ol derivatives

Cholest-4α-methyl-7-en-3β-ol (1) has potent inhibitory activity against pc 12 tumor with 0.5043 ratio (10 μg/mL). This paper describes a series of structural modification of this compound, which focus on 3β-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-4α-methyl-8-en-3β,7α-diol 6a inhibits KB cell significantly with IC50 1.32 × 10−9 μg/mL. In addition, the cytotoxic properties of this compound against HCT-8 and BEL-7402 are excellent with IC50 1.2 μg/mL.