Publisher Summary This chapter provides a brief review on uracil and its chemistry, by no means exhaustive, has pointed out by some selective but typical examples that show uracils and their derivatives possess considerable synthetic potential. In most cases, a few easy reaction steps enable the synthesis of novel and highly interesting types of condensed heterocycles that are difficult to obtain by other synthetic means.

Uracils: Versatile Starting Materials in Heterocyclic Synthesis

Regiospecific one-pot synthesis of pyrimido[4,5-d]pyrimidine derivatives in the solid state under microwave irradiations.

Polo-like kinase 1 (PLK1) has been shown to be involved in cell cycle progression of rapidly proliferating, nontransformed cells as well as tumor cells. In cancer, overexpression of PLK1 contributes to the malignant state by aberrant cell cycle regulation at the G2/M phase. We attempted to validate PLK1 function in cell-based assays using antisense oligonucleotide knockout approaches. Our own results and published findings of other groups have led to the conclusion that PLK1 is a logical point for pharmacological intervention. HTS campaigns performed against the recombinant PLK1-protein led to the identification of two PLK1 inhibitory scaffolds, one containing a 7-azapteridine ring system, the other a fused tetracyclic ketone system. These compounds showed low micromolar antiproliferative activity towards SW620, a human colon cancer cell line, most likely through cell cycle arrest at the G2/M phase. Our data suggest that PLK1 may serve as a target for discovering small molecule anticancer agents. Drug Dev. Res. 62:349–361, 2004. © 2004 Wiley-Liss, Inc.

PLK1 as a potential drug target in cancer therapy

A novel synthesis of 3-(substituted)pyrimido[4,5-c]pyridazine-5,7(1H,6H)-diones

A variety of different compounds of fused uracils were prepared simply by the heating of 6-hydrazinyl-1-methyl-, 6-hydrazinyl-1-propyl-, or 6-hydrazinyl-1,3-dipropyluracil under reflux with ninhydrin, isatin, benzylidene malononitrile, benzylylidene ethyl cyanoacetate, benzil, and phenacyl bromide derivatives. The newly synthesized compounds were completely screened for antimicrobial and antitumor activity.

https://www.mdpi.com/1420-3049/21/12/1714/pdf

Phillip Dan Cook

Papers

The synthesis of pyrimido[4,5-c] pyridazines and pyrido[2,3-d]pyrimidines related to toxoflavin and fervenulin