（四氢-β-咔啉）-1,3,5-三嗪类化合物的合成及细胞毒性评价作为抗癌剂。
Synthesis and cytotoxicity evaluation of (tetrahydro-beta-carboline)-1,3,5-triazine hybrids as anticancer agents.
机构信息
Division of Medicinal & Process Chemistry, Central Drug Research Institute, CSIR, Lucknow 226001, India.
出版信息
Eur J Med Chem. 2010 Jun;45(6):2265-76. doi: 10.1016/j.ejmech.2010.02.001. Epub 2010 Feb 10.
A series of tetrahydro-beta-carbolines and 1,3,5-triazine hybrids have been synthesized and evaluated for their cytotoxicity against a panel of eight human cancer cell lines and normal human fibroblasts (NIH3T3). It led us to discovery of racemic compounds 69, 71 and 75, which are selectively cytotoxic towards KB (oral cancer) cell line with IC50 values of 105.8, 664.7 and 122.2 nM, respectively; while their enantiopure forms are less active and not selective. Enantiopure compound 42 showed 2.5 times more selectivity towards MCF7 cells over normal fibroblast NIH3T3 cells with an IC50 value of 740 nM, also arrests cell cycle in G1 phase and induces apoptosis in MCF7 and MDA MB231 cell lines.
一系列四氢-β-咔啉和 1,3,5-三嗪类化合物已被合成，并评估了它们对八种人癌细胞系和正常成纤维细胞（NIH3T3）的细胞毒性。这使我们发现了外消旋化合物 69、71 和 75，它们对 KB（口腔癌）细胞系具有选择性细胞毒性，IC50 值分别为 105.8、664.7 和 122.2 nM；而它们的对映体纯形式活性较低且无选择性。对映体纯化合物 42 对 MCF7 细胞的选择性是对正常成纤维细胞 NIH3T3 细胞的 2.5 倍，IC50 值为 740 nM，还能使 MCF7 和 MDA MB231 细胞系的细胞周期停滞在 G1 期并诱导细胞凋亡。
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