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