邻碳硼烷氧基-1,3,5-三嗪衍生物的合成、表征、X 射线结构研究及生物活性。

School of Pharmacy, Jiangsu University, Zhenjiang 212013, Jiangsu, China.

Metabolic Regulation Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 34141, Korea.

Molecules. 2018 Aug 30;23(9):2194. doi: 10.3390/molecules23092194.

Morpholine- and bis(2-methoxyethyl)amine-substituted 1,3,5-triazine derivatives containing an alkoxy-o-carborane in the 6-position of the triazine ring were successfully synthesized. The molecular structures of the methoxy- and ethoxy-o-carboranyl-1,3,5-triazines were established by X-ray crystallography. In vitro studies showed that the methylene bridged morpholine- and bis(2-methoxyethyl)amine-substituted o-carboranyl-1,3,5-triazines accumulated to high levels in B16 melanoma cells and exhibited higher cytotoxicity than p-boronophenylalanine.

成功合成了 6-位取代烷氧基-o-卡硼烷的吗啉基和双（2-甲氧基乙基）胺取代的 1,3,5-三嗪衍生物。通过 X 射线晶体学确定了甲氧基和乙氧基-o-卡硼烷-1,3,5-三嗪的分子结构。体外研究表明，亚甲基桥连的吗啉基和双（2-甲氧基乙基）胺取代的 o-卡硼烷-1,3,5-三嗪在 B16 黑色素瘤细胞中积累到很高水平，并表现出比硼替佐米更高的细胞毒性。