Jin Guofan, Xiao Fuyan, Liu Ruijiang
School of Pharmacy, Jiangsu University, Zhenjiang, 212013, People's Republic of China.
Chem Cent J. 2018 Jun 29;12(1):76. doi: 10.1186/s13065-018-0444-z.
(Z,Z')-1,1'-(4-ortho-Caboranyldimethyl)-bis(2-methoxyphenylethan-1-oxime) intermediate 3 was synthesized by a three-step reaction with a final treatment with base to give a new series of ortho-carboranyl biphenyloxime derivatives (4-8). Compounds 7 and 8 showed high solubility and the in vitro study results revealed high levels of accumulation in HeLa cells with higher cytotoxicity and boron uptake compared to L-boronphenylalanine.
(Z,Z')-1,1'-(4-邻碳硼烷基二甲基)-双(2-甲氧基苯乙酮肟)中间体3通过三步反应合成,最后用碱处理得到一系列新的邻碳硼烷基联苯肟衍生物(4-8)。化合物7和8显示出高溶解度,体外研究结果表明,与L-硼苯丙氨酸相比,它们在HeLa细胞中的积累水平较高,具有更高的细胞毒性和硼摄取量。