Heterocyclic amplifiers of phleomycin. I. Some pyrimidinylpurines, pyrimidinylpteridines and phenylpyrimidines

Abstract

Synthetic routes are described to 5,6-diamino-2,4'-bipyrimidin-4-ones and thence to 2-(pyrimidin-4'-yl)purines and 2-(pyrimidin-4'-yl)pteridines, some of which bear a sulfur- or nitrogen-linked basic side chain; also reported are routes to a series of phenyl- and diphenyl-pyrimidines, to each of which is attached a similar sulfur-, nitrogen-, or oxygen-linked side chain. Members of all the above systems show activity as amplifiers of phleomycin in a bacterial screen but the phenylpyrimidines with a sulfur-linked side chain are especially active.