106511-81-3Relevant academic research and scientific papers
Synthesis, antitumor activity and molecular docking study of some novel 3-benzyl-4(3H)quinazolinone analogues
Al-Suwaidan, Ibrahim A.,Abdel-Aziz, Alaa A.-M.,Shawer, Taghreed Z.,Ayyad, Rezk R.,Alanazi, Amer M.,El-Morsy, Ahmad M.,Mohamed, Menshawy A.,Abdel-Aziz, Naglaa I.,El-Sayed, Magda A.-A.,El-Azab, Adel S.
, p. 78 - 89 (2016/01/15)
A novel series of 3-benzyl-substituted-4(3H)-quinazolinones were designed, synthesized and evaluated for their in vitro antitumor activity. The results of this study demonstrated that 2-(3-benzyl-6-methyl-4-oxo-3,4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl)acetamide, 2-(3-benzyl-6,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl)acetamide and 3-(3-benzyl-6-methyl-4-oxo-3,4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl)-propanamide have shown amazing broad spectrum antitumor activity with mean GI50 (10.47, 7.24 and 14.12 μM. respectively), and are nearly 1.5-3.0-fold more potent compared with the positive control 5-FU with mean GI50, 22.60 μM. On the other hand, compounds 6 and 10 yielded selective activities toward CNS, renal and breast cancer cell lines, whereas compound 9 showed selective activities towards leukemia cell lines. Molecular docking methodology was performed for compounds 7 and 8 into ATP binding site of EGFR-TK which showed similar binding mode to erlotinib, while compound 11 into ATP binding site of B-RAF kinase inhibited the growth of melanoma cell lines through inhibition of B-RAF kinase, similar to PLX4032.
A New Synthesis of 1,3,4-Thiadiazoloquinazolin-5-ones
Pathak, U. S.,Devani, M. B.,Shishoo, C. J.,Kulkarni, R. R.,Rakholia, V. M.,et al.
, p. 489 - 491 (2007/10/02)
A new synthesis of 3-amino-2-mercaptoquinazolin-4-one (4) and its cyclization to thiadiazoloquinazolines by reaction with one carbon donors is reported.
