Abstract
A series of novel nucleosides containing 1,2,4-triazine and pyrrole moieties were efficiently prepared and characterized via analytical, spectral, and computational methods. The synthesized compounds had no effect on human immunodeficiency virus type 1 (HIV-1) (HTLV IIIB). Moreover, the triazine derivatives 8a and 8b were screened for their anticancer activity against five human cancer types [breast adenocarcinoma (MCF-7), pancreatic carcinoma (Paca2), lung carcinoma (A-549), human bone cancer cell line (Hos), and a normal human (BJ-1)] cell lines using MTT assay. The obtained results revealed that the tested nucleosides 8a and 8b had significant inhibitory activity against Paca2, but no activity against A-549, Hos, and BJ-1 cell lines. The structure-activity relationship displayed an increase in anticancer potential of compound 8a with the increase of number of hydrogen bond interactions with Lys 89 as the key interactive amino acid of CDK-2 kinase.
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