150450-42-3Relevant articles and documents
Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
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, (2008/06/13)
Derivatives of quinazoline are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit the growth of neoplastic cells.
Anti-ischemic 2,4-diaminoquinazolines
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, (2008/06/13)
The invention is directed to certain 2,4-diaminoquinazoline compounds, their pharmaceutically acceptable salts, the pharmaceutical compositions comprising those compounds and their therapeutic methods of use. The compounds possess anti-ischemic activity.
Cyclic GMP Phosphodiesterase Inhibitors. 2. Requirement of 6-Substitution of Quinazoline Derivatives for Potent and Selective Inhibitory Activity
Takase, Yasutaka,Saeki, Takao,Watanabe, Nobuhisa,Adachi, Hideyuki,Souda, Shigeru,Saito, Isao
, p. 2106 - 2111 (2007/10/02)
We synthesized various 4-amino>quinazolines substituted at the 5- to 8-positions and evaluated their inhibitory activities toward cyclic GMP phosphodiesterase (cGMP-PDE) from porcine aorta.Monosubstitution at the 6-position was essential for the inhibitory activity, and the preferred substituents were compact and hydrophobic: methoxy (3b, IC50 = 0.23 μM), methyl (3c, 0.10 μM), chloro (3d, 0.019 μM), thiomethyl (3f, 0.031 μM), and cyano (3p, 0.090 μM) groups.Compounds 3b-d, f, p lacked inhibitory activity toward other PDE isozymes (all IC50 values > 100 μM), and their relaxing activities in porcine coronary arteries were well correlated with the inhibitory activities toward cGMP-PDE (r = 0.88, p 0.05).One of these compounds, 3b, elevated the intracellular cGMP level in isolated porcine coronary arteries without causing any change in the cAMP level.We consider that this series of compounds dilates coronary arteries via potent and specific inhibition of cGMP-PDE.