80195-32-0Relevant academic research and scientific papers
Synthesis, antitumor and antimicrobial activity of some new 6-methyl-3-phenyl-4(3H)-quinazolinone analogues: in silico studies
Alanazi, Amer M.,Abdel-Aziz, Alaa A.-M.,Shawer, Taghreed Z.,Ayyad, Rezk R.,Al-Obaid, Abdulrahman M.,Al-Agamy, Mohamed H. M.,Maarouf, Azza R.,El-Azab, Adel S.
, p. 721 - 735 (2016/07/07)
Some new derivatives of substituted-4(3H)-quinazolinones were synthesized and evaluated for their in vitro antitumor and antimicrobial activities. The results of this study demonstrated that compound 5 yielded selective activities toward NSC Lung Cancer EKVX cell line, Colon Cancer HCT-15 cell line and Breast Cancer MDA-MB-231/ATCC cell line, while NSC Lung Cancer EKVX cell line and CNS Cancer SF-295 cell line were sensitive to compound 8. Additionally, compounds 12 and 13 showed moderate effectiveness toward numerous cell lines belonging to different tumor subpanels. On the other hand, the results of antimicrobial screening revealed that compounds 1, 9 and 14 are the most active against Staphylococcus aureus ATCC 29213 with minimum inhibitory concentration (MIC) of 16, 32 and 32 μg/mL respectively, while compound 14 possessed antimicrobial activities against all tested strains with the lowest MIC compared with other tested compounds. In silico study, ADME-Tox prediction and molecular docking methodology were used to study the antitumor activity and to identify the structural features required for antitumor activity.
Novel 4(3H)-quinazolinone analogs: Synthesis and anticonvulsant activity
El-Azab, Adel S.,Abdel-Hamide, Sami G.,Sayed-Ahmed, Mohamed M.,Hassan, Ghada S.,El-Hadiyah, Tariq M.,Al-Shabanah, Othman A.,Al-Deeb, Omar A.,El-Subbagh, Hussein I.
, p. 2815 - 2827 (2013/07/26)
A new series of quinazoline analogs was designed, synthesized, and evaluated for their anticonvulsant activity. Compounds 6, 12, 21, 36, 37, and 38 showed 70-100 % protection against PTZ-induced seizures acting as GABA A receptor agonists. Compound N-(3,4,5,6-tetrachloro-phthalimido)-2- [(3-phenyl-4-oxo-6-methyl-3H-quinazolin-2-yl)-thio]acetamide (12) representing the moderate active compounds and 2-[6-iodo-4-oxo-2-(thiophen-2-yl)-quinazolin- 3(4H)-yl]-isoindoline-1,3-dione (38) representing the remarkably active compounds in this stud, showed ED50 values of 457 and 251 mg/kg; TD50 values of 562 and 447 mg/kg; PI values of 1.22 and 1.78, LD 50 values of 1,288 and 1,380 mg/kg, and TI values of 2.82 and 5.50, respectively. Compound 38 proved to be almost twofold more active than the standard drug sodium valproate.
