Institute of Pharmaceutical Chemistry and, MTA-SZTE Stereochemistry Research Group, Hungarian Academy of Sciences, University of Szeged, Eötvös u. 6, 6720, Szeged, Hungary.
Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, 6720, Szeged, Hungary.
ChemistryOpen. 2022 Oct;11(10):e202200169. doi: 10.1002/open.202200169.
A series of novel heterocyclic structures, namely 1,3-oxazines, 1,3-thiazines and 2,4-diaminopyrimidines, were designed and synthesised. The bioassay tests demonstrated that, among these analogues, 2,4-diaminopyridine derivatives showed significant antiproliferative activity against different human cancer cell lines (A2780, SiHa, HeLa, MCF-7 and MDA-MB-231). Pyrimidines substituted with N -(p-trifluoromethyl)aniline, in particular, displayed a potent inhibitory effect on the growth of cancer cells. Structure-activity relationships were also studied from the aspects of stereochemistry on the aminodiol moiety as well as exploring the effects of substituents on the pyrimidine scaffold.
一系列新型杂环结构，即 1,3-恶嗪、1,3-噻嗪和 2,4-二氨基嘧啶，被设计和合成。生物测定试验表明，在这些类似物中，2,4-二氨基吡啶衍生物对不同的人癌细胞系（A2780、SiHa、HeLa、MCF-7 和 MDA-MB-231）表现出显著的抗增殖活性。嘧啶用 N-(对三氟甲基)苯胺取代，特别是对癌细胞的生长具有很强的抑制作用。还从氨基二醇部分的立体化学以及探索嘧啶支架上取代基的影响等方面研究了构效关系。
