摘要
The current interest of the team has been focused on investigation of novel amides with potential cytotoxicity. The presented series of compounds was synthesized from selected steryl hemiesters and hetero-aromatic amines. The synthetic protocol was designed in a simple and economic way, and divided into several general methodologies applicable to the compounds synthesized. The cytotoxicity was tested on cells derived from human T-Iymphoblastic leukemia, breast adenocarcinoma and cervical cancer, and compared with tests on normal human fibroblasts. Most of the lanosterol-based compounds (3-5 and 7-10) showed medium to good cytotoxicity, while only two derivatives of cholesterol (18 and 19) showed medium cytotoxicity on human T-Iymphoblastic leukemia cell line. The compounds 8 and 9 displayed the reasonable cytotoxicity among this series of amides, tested on the cell lines of T-Iymphoblastic leukemia [14.5 +/- 0.4 mu M (8) and 18.5 +/- 3.9 mu M (9)], breast adenocarcinoma [19.5 +/- 2.1 mu M (8) and 23.1 +/- 4.0 mu M (9)] and cervical cancer [24.8 +/- 5.3 mu M (8) and 29.1 +/- 4.7 mu M (9)]. Only the compound 8 was adequately less active on normal human fibroblasts (40.4 +/- 11.1 mu M).
- 出版日期2013-12-20