División de Estudios de Posgrado, Maestría en Ciencias Químicas, Universidad del Papaloapan, Circuito Central 200, Col. Parque Industrial, Tuxtepec, 68301 Oaxaca, Mexico.
Centro de Investigaciones Científicas, Instituto de Química Aplicada, Universidad del Papaloapan, Circuito Central 200, Col. Parque Industrial, Tuxtepec, 68301 Oaxaca, Mexico.
Steroids. 2022 Jun;182:109012. doi: 10.1016/j.steroids.2022.109012. Epub 2022 Mar 16.
Using cholesterol and diosgenin as starting materials, we have designed a straightforward methodology to prepare in a reduced number of steps a novel series of steroidal oximes and their aza-homolactam analogs with four types of side chains: cholestane, spirostane, 22-oxocholestane and 22,26-epoxycholestene. The products were evaluated for their cytotoxic activity against the MCF-7 breast cancer cell line. Moreover, the selectivity of the most active compounds was determined against peripheral blood lymphocytes. Compounds 5, 8 and 13 were found to be the most active derivatives, exhibiting IC values in the low micromolar range (7.9-9.5 µM) and excellent selectivities (IC > 100 µM) against the non-tumor cell line.
以胆固醇和薯蓣皂素为起始原料，我们设计了一种简洁的方法，通过较少的步骤制备了一系列新型甾体肟及其四种类侧链的氮杂内酰胺类似物：胆甾烷、螺甾烷、22-氧代胆甾烷和 22,26-环氧胆甾烯。评估了这些产物对 MCF-7 乳腺癌细胞系的细胞毒性活性。此外，还测定了最活跃化合物对外周血淋巴细胞的选择性。发现化合物 5、8 和 13 是最活跃的衍生物，其 IC 值在低微摩尔范围内（7.9-9.5µM），对非肿瘤细胞系具有优异的选择性（IC>100µM）。
