Abstract

A series of novel hybrids of indole-pyrimidine moieties were synthesized and evaluated for their in vitro anti-cancer, in vitro anti-bacteria and in vitro anti-fungal activities. The results showed that most of these compounds possessed significant cytotoxic potency against four cancer cell lines, HeLa, HEK 293T and MCF-7. The compounds 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine,4-(4-chlorophenyl)-6-(1-methyl-1H-indol-3-yl) pyrimidin-2-amine and4-(1H-indole-3-yl)-6-phenylpyrimidin-2-amine showed good activity against HEK 293T. The compounds 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine and 4-(4-chlorophenyl)-6-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine showed good to moderate activity against MCF-7, whereas compound 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine exhibit moderate activity against HaLa S3 cell line. The newly synthesized derivatives were also screened for their in vitro anti-bacterial activity against Bacillus subtilis, B. megatherium, B. pumilis, Proteus mirabilis, Klebsiella pneumoniae, Enterobacter aerogenes, Streptococcus pyogenes, Staphylococcus aureus, Proteus vulgaris, Escherichia coli, using streptomycin as a standard drug. Among tested compound 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine shows more potent activity compared to standard, where as the remaining analogues exhibited well to moderate activity compared to standard. Anti-fungal screening results suggest that the compound 4-(4-chlorophenyl)-6-(1H-indol-3-yl)pyrimidin-2-amineshowed potent activity against Dreschleria halides. The remaining compounds showed nearest activity against all the tested fungal strains compared to standard drug.

中文翻译：

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作为有效抗癌和抗微生物药物的新型吲哚-嘧啶衍生物的一锅多组分合成和生物学评价

摘要

合成了一系列吲哚-嘧啶部分的新型杂化物，并评估了它们的体外抗癌、体外抗菌和体外抗真菌活性。结果表明，这些化合物中的大多数对四种癌细胞系 HeLa、HEK 293T 和 MCF-7 具有显着的细胞毒性。化合物4-(3-(苄氧基)苯基)-6-(1-甲基-1H-吲哚-3-基)嘧啶-2-胺，4-(4-氯苯基)-6-(1-甲基- 1 H -indol-3-yl)pyrimidin-2-amine和4-(1 H -indole -3-yl)-6-phenylpyrimidin-2-amine对HEK 293T表现出良好的活性。化合物4-(3-(苄氧基)苯基)-6-(1-甲基-1H-吲哚-3-基)嘧啶-2-胺和4-(4-氯苯基)-6-(1-甲基- 1小时-indol-3-yl)pyrimidin-2-amine 对 MCF-7 表现出良好到中等的活性，而化合物 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1 H -indol-3-yl )pyrimidin-2-amine 对 HaLa S3 细胞系表现出中等活性。新合成的衍生物还筛选了对它们的体外抗细菌活性的枯草芽孢杆菌，B.大地懒，B.短小，奇异变形杆菌，肺炎克雷伯菌，产气肠杆菌，化脓性链球菌，金黄色葡萄球菌，变形杆菌，大肠埃希氏菌，使用链霉素作为标准药物。在测试化合物中，4-(3-(苄氧基)苯基)-6-(1-methyl-1 H -indol-3-yl)pyrimidin-2-amine 显示出比标准品更有效的活性，而其余类似物表现良好与标准相比适度活动。抗真菌筛选结果表明，化合物4-（4-氯苯基）-6-（1- ħ -吲哚-3-基）嘧啶-2- amineshowed有效的活性抗Dreschleria卤化物。与标准药物相比，其余化合物对所有测试的真菌菌株表现出最接近的活性。