(Open access funding provided by University of Szeged)
Subjects:
Pharmacology and pharmacy
Chemical sciences
Organic chemistry
Synthetic Organic chemistry
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-2-(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.
