Abstract

In the present paper we synthesized 10 unique pyrimidine scaffolds (Lanso Aminopyrimidines) derived from 4-(2,2,2-trifluoroethoxy)-2-(chloromethyl)-3-methylpyridine as a core molecule, which can be used for the design of more potent and effective anticancer agents. The in vitro anticancer activities of the synthesized new pyrimidine derivatives were screened at the National Cancer Institute, USA, against a full NCI 60 cell lines. Most of the compounds exhibited remarkable growth inhibition at a single dose (10 µM) in Leukaemia cancer cell. 4-(4-{3-Methyl-4-[(2,2,2-trifluoroethoxy)pyridin-2-yl]methylamino}phenyl)-6-phenyl-1,6-dihydropyrimidin-2-amine which showed high activity against RPMI-8226 leukaemia cancer cells (GI₅₀ 35.50 µM) and can be considered as a candidate lead compound for developing new promising anticancer agents.

中文翻译：

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Lanso氨基嘧啶类化合物作为白血病的主要化学治疗剂的合成

摘要

在本文中，我们合成了以4-（2,2,2-三氟乙氧基）-2-（氯甲基）-3-甲基吡啶为核心分子的10种独特的嘧啶支架（Lanso Aminopyrimidines），可用于设计更有效的抗癌药。合成的新嘧啶衍生物的体外抗癌活性在美国国家癌症研究所针对完整的NCI 60细胞株进行了筛选。大多数化合物在白血病癌细胞中以单剂量（10 µM）表现出显着的生长抑制作用。显示出高活性的4-（4- {3-甲基-4-[（2,2,2-三氟乙氧基）吡啶-2-基]甲基氨基}苯基）-6-苯基-1,6-二氢嘧啶-2-胺抵抗RPMI-8226白血病细胞（GI ₅₀ 35.50 µM），可以被视为开发新的有前途的抗癌药物的候选先导化合物。