127105-49-1Relevant articles and documents
Quinazoline thymidylate synthase inhibitors
-
, (2008/06/13)
The invention relates to quinazoline derivatives or pharceutically-acceptable salts thereof, which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: STR1 wherein R1 is (1-4C)alkyl; the quinazoline ring may optionally bear one or two further substituents selected from halogeno, (1-4C)alkyl and (1-4C)alkoxy; R2 is hydrogen or (1-4C)alkyl; R3 includes hydrogen and (1-4C)alkyl; and Ar is optionally substituted phenylene or heterocyclene; or a pharmaceutically-acceptable salt or ester thereof.
Non-glutamate type pyrrolo[2,3-d]pyrimidine antifolates. I: Synthesis and biological properties of pyrrolo[2,3-d]pyrimidine antifolates containing tetrazole congener of glutamic acid
Itoh,Yukishige,Wajima,Ootsu,Akimoto
, p. 230 - 235 (2007/10/02)
Either the α- or γ-carboxyl group of the glutamic acid moiety of N-[4-[3-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)propyl] benzoyl]-L-glutamic acid (1b, TNP-351) and its related compound (1a) was replaced with a 1H-tetrazole ring, and the in
