3β-Hydroxy-6-aza-cholestane and related analogues as phosphatidylinositol specific phospholipase C (PI-PLC) inhibitors with antitumor activity

…, LH Zalkow, YH Li, C Zhu, G Powis, M Kunkel

文献索引：Xie; Peng; Zalkow; Li; Zhu; Powis; Kunkel Bioorganic and medicinal chemistry, 2000 , vol. 8, # 4 p. 699 - 706

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被引用次数: 21

摘要

6-Aza steroid analogues were synthesized as PI-PLC inhibitors. The most active compound, 3β-hydroxy-6-aza-cholestane (1) showed potent PI-PLC inhibition (IC50= 1.8 μM), similar to that of the commercially available steroid analogue U73122 (IC50= 1–2.1 μM). Compound 1 exhibited significant growth inhibition effects (IC50= 1.3 μM in each case) against MCF-7 and HT-29 cancer cells in in vitro cell culture. Compound 1 also inhibited the in vitro ...