Bioorganic chemistry

Activity of 6-aryl-pyrrolo [2, 3-d] pyrimidine-4-amines to Tetrahymena

SJ Kaspersen, E Sundby, C Charnock, BH Hoff

Index: Kaspersen, Svein Jacob; Hoff, Bard Helge; Sundby, Eirik; Charnock, Colin Bioorganic Chemistry, 2012 , vol. 44, p. 35 - 41,7

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Citation Number: 12

Abstract

A series 6-aryl-pyrrolo [2, 3-d] pyrimidine-4-amines (43 compounds), some of which are epidermal growth factor tyrosine kinase inhibitors, were tested for their protozoal toxicity using an environmental Tetrahymena strain as model organism. The protozoacidal activity of the analogues was found to be highly dependent on a 4-hydroxyl group at the 6-aryl ring, and a chiral 1-phenylethanamine substituent in position 4. Further, the potency was ...