Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
Here, we investigated the structure-activity relationships of the 6,7-dimethoxyquinazoline moiety. With regard to exploration of positions and varieties of substituents on the quinazoline ring, 6,7-dialkoxy substitution was optimal. This study suggests the possibility of further modifications for this moiety.
Matsuno
Kenji
K
Kyowa Hakko Kogyo Co., Ltd., Pharmaceutical Research Institute, Shimotogari 1188, Nagaizumi-cho, Sunto-gun, Shizuoka 411-8731, Japan. k.matsuno@teijin.co.jp
Seishi
Takashi
T
Nakajima
Takao
T
Ichimura
Michio
M
Giese
Neill A
NA
Yu
Jin-Chen
JC
Oda
Shoji
S
Nomoto
Yuji
Y
D000818:Animals; D006801:Humans; D020128:Inhibitory Concentration 50; D010766:Phosphorylation / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017479:Receptors, Platelet-Derived Growth Factor / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D011799:Quinazolines; D017479:Receptors, Platelet-Derived Growth Factor