76857-06-2Relevant articles and documents
Synthesis and evaluation of anticancer and PDE 5 inhibitory activity of spiro-substituted quinazolin-4-ones
Ameen, Mohamed A.,Ahmed, Essam Kh.,Ramadan, Mohamed,Abd El-Naby, Hisham A.,Abdel-Haseeb, Asmaa A.
, p. 1513 - 1523 (2017/07/18)
A series of novel spiro-substituted 2,3-dihydroquinazolin-4(1H)-ones was synthesized and structurally confirmed by spectral analysis, screened for their anticancer activity at a concentration of 10 μΜ against a panel of 56 cell lines derived from nine different types of cancers, including leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers. The synthesized compounds screened for their PDE 5 inhibitory activity and it showed encouraged activity compared to sildenafil. Graphical abstract: [Figure not available: see fulltext.].
Facile method for the combinatorial synthesis of 2,2-Disubstituted Quinazolin-4(1 H)-one derivatives catalyzed by iodine in ionic liquids
Wang, Xiang-Shan,Yang, Ke,Zhou, Jie,Tu, Shu-Jiang
scheme or table, p. 417 - 421 (2010/09/05)
A mild and facile method for the combinatorial synthesis of quinazolin-4-(1H)-one derivatives, containing simple 2,2-disubstituted quinazolin-4-(1H)-ones, spirocyclic quinazolin-4-(1H)-ones, spiro-heterocyclic quinazolin-4-(1H)-ones, and dispirocyclic quinazolin-4-(1H)-ones, is described, which results in high yields by using ionic liquids as green media. The method involves the reaction of 2-aminobenzamides with various ketones catalyzed by iodine and provides new quinazolin-4-(1H)-one library for biomedical screening.
Synthesis of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines as potential antihypertensive agents
Takai,Obase,Nakamizo,Teranishi,Kubo,Shuto,Kasuya,Shigenobu,Hashikami,Karashima
, p. 1116 - 1128 (2007/10/02)
A series of 1- and 3-(1-substituted 4-piperidinyl)-1,2,3,4-tetrahydro-2-oxoquinazolines were synthesized and tested for antihypertensive activity. Among the compounds tested, 1-(2-hydroxy-2-phenethyl)-4-(1,2,3,4-tetrahydro-2-oxo-3-quinazolinyl) piperidine derivatives were generally the most effective in lowering blood pressure in the spontaneous hypertensive rat model. Of these, 1-[2-(4-chlorophenyl)-2-hydroxyethyl]-4-(1,2,3,4-tetrahydro-2-oxo-3- quinazolinyl)piperidine (KF5908) seemed the most promising.