Abstract

Novel 2-amino(substituted pyrimidin-2-yl)benzimidazole and 2-amino-3,4-dihydro[1,3,5]triazino[1,2-a]benzimidazole hybrids were synthesized and evaluated for their in vitro antitumor activity at National Cancer Institute (NCI), against 60 human cell lines for primary anticancer screening. Among the tested compounds, 8 and 23 exhibited significant growth inhibition. Compound 8 was very promising anticancer; therefore, this compound passed on to further evaluation at five concentration levels (0.01–100 uM), and it showed potent activity in five-dose testing. Detailed synthesis, spectroscopic, and biological data are reported.

摘要

合成了新型 2-氨基（取代的嘧啶-2-基）苯并咪唑和 2-氨基-3,4-二氢[1,3,5]三嗪[1,2- a ]苯并咪唑杂化物，并评估了它们的体外抗肿瘤活性在美国国家癌症研究所 (NCI)，针对 60 种人类细胞系进行初级抗癌筛查。在测试的化合物中，8和23表现出显着的生长抑制。化合物8是非常有前景的抗癌药；因此，该化合物在五个浓度水平（0.01-100 uM）下进行了进一步评估，并且在五剂量测试中显示出有效的活性。报告了详细的合成、光谱和生物学数据。