Pyrimidine Derivatives with Terminal Pyridyl Heterocycles: Facile Synthesis and Their Antiproliferative Activities

Abstract

Incorporation of heterocyclic pyrimidine or pyridine motifs is common in the drug design for various therapeutic applications. Herein, we describe the facile synthesis of two molecules containing both pyrimidine and pyridine scaffolds. A variety of analytical techniques (multinuclear NMR, Fourier transform infrared, and mass spectrometry analyses) confirmed the purity of these molecules. In pristine form, their potential as antitumor drugs was screened by investigating their cytotoxicity against various cell lines (cancerous and normal cells). Experimental results confirmed that the two molecules exhibited cell growth inhibition at very low concentrations. This was evident from their IC50 values that are in the range of 0.45–2.20 μM.

Access to Highly Substituted Pyrimidine N-Oxides and 4-Acetoxymethyl-Substituted Pyrimidines via the LANCA Three-Component Reaction–Cyclocondensation Sequence

“…Pyrimidines constitute one of the most important classes of nitrogen-containing heterocycles and play a prominent role in organic synthesis as well as in medicinal and agrochemistry. 1 The pyrimidine core is for instance present in pharmacologically interesting compounds possessing antitubercular, 2 antiproliferative, 3 and CYP1A2 inhibitory activities. 4 Derivatives of pyrimidines are identified as potent dual M3 antagonists and PDE4 inhibitors 5 and more recently they have been tested in multiple phase I/II trials for treatment of cancer.…”