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Heterocondensed quinazolones: synthesis and protein-tyrosine kinase inhibitory activity of 3,4-dihydro-1H,6H-[1,4]oxazino-[3,4-b]quinazolin-6-one derivatives

✍ Scribed by Lászlo Ôrfi; József Kökösi; György Szász; István Kövesdi; Marianna Mák; István Teplán; György Kéri


Book ID
103992271
Publisher
Elsevier Science
Year
1996
Tongue
English
Weight
365 KB
Volume
4
Category
Article
ISSN
0968-0896

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✦ Synopsis


1-Benzylidene (2-14) and 1-phenylhydrazono derivatives (15-29) of 3,4-dihydro-1H,6H-[1,4]oxazino[3,4-b]quinazolin-6-one (1) were obtained from the condensation reactions of 1 with a series of aromatic aldehydes and by direct diazonium coupling with aryl-diazonium chlorides. The substances were tested for their ability to inhibit the tyrosine kinase activity of SW-620 (human colon carcinoma) cells. Compounds 8, 10, 12 and 13 showed remarkable inhibitory activity.


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## Abstract magnified image The 2‐amino‐4‐(het)aryl‐4,6‐dihydro‐1(3)(11)__H__‐[1,3,5]triazino[2,1‐__b__]quinazolin‐6‐ones were prepared readily by cyclocondensation of anthranilic acid derived 4‐oxo‐3,4‐dihydroquinazolinyl‐2‐guanidine with a variety of aldehydes. The structures of the compounds we