37856-23-8Relevant academic research and scientific papers
Synthesis, in silico and in vitro assessment of new quinazolinones as anticancer agents via potential AKT inhibition
Abdelmonsef, Aboubakr H.,Donia, Thoria,El-Naggar, Mohamed,Noser, Ahmed A.
, (2020)
A series of novel quinazolinone derivatives (2–13) was synthesized and examined for their cytotoxicity to HepG2, MCF-7, and Caco-2 in an MTT assay. Among these derivatives, compounds 4 and 9 exhibited significant cytotoxic activity against Caco-2, HepG2, and MCF-7 cancer cells. Compound 4 had more significant inhibitory effects than compound 9 on Caco-2, HepG2, and MCF-7 cell lines, with IC50 values of 23.31 ± 0.09, 53.29 ± 0.25, and 72.22 ± 0.14μM, respectively. The AKT pathway is one of human cancer’s most often deregulated signals. AKT is also overexpressed in human cancers such as glioma, lung, breast, ovarian, gastric, and pancreas. A molecular docking study was performed to analyze the inhibitory action of newly synthetic quinazolinone derivatives against Homo sapiens AKT1 protein. Molecular docking simulations were found to be in accordance with in vitro studies, and hence supported the biological activity. The results suggested that compounds 4 and 9 could be used as drug candidates for cancer therapy via its potential inhibition of AKT1 as described by docking study.
Synthesis and antimicrobial evaluation of quinazoline-4[3h]-one derivatives
Chaudhary, Cheenu,Hashim, S. Riaz,Kumar, Surendra,Kumar, Sushil
, p. 547 - 554 (2021/07/25)
The present investigation aimed to synthesize quinazoline-4(3H)-one derivatives (B1-10) and evaluated their antimicrobial activity. The test compounds (B1-10) were obtained by reaction of 2-phenyl-4H-benzo[d] [1, 3]oxazin-4-one (1) with 4-aminophenol (2)
Design, synthesis and in vivo screening of some novel quinazoline analogs as anti-hyperlipidemic and hypoglycemic agents
Mokale, Santosh N.,Palkar, Akash D.,Dube, Pritam N.,Sakle, Nikhil S.,Miniyar, Pankaj B.
supporting information, p. 272 - 276 (2016/01/09)
A novel series of substituted quinazoline derivatives were designed, synthesized and evaluated for their hypolipidemic activity in cholesterol induced hyperlipidemic rats. In vivo screening concluded that compounds A-4, C-5 and C-6 have shown potent antihyperlipidemic activity by decreasing the plasma level of triglycerides (TG), very low density lipoprotein (VLDL), low density lipoprotein (LDL), followed by increase in level of high density lipoprotein (HDL).
Syntheses of new heterocycles derived from 2-phenyl-3,1-benzoxazin-4-one and their antibacterial and antifungal activity
Havaldar, Freddy H.,Patil, Abhay R.
experimental part, p. 251 - 261 (2010/07/10)
A series of novel substituted N-(6-substituted-4H-benzo[e][1,3]oxazin-3-yl) - 2-[4-(4-oxo-2-phenyl-4H-quinazolin-3-yl)-phenoxy]-acetamides (9a-b) and N-(6-substituted-2-thione-4H-benzo[e][1,3]oxazin-3-yl)-2-[4-(4-oxo-2-phenyl-4H- quinazolin-3-yl)-phenoxy]
Syntheses of some novel [4-(4-oxo-2-phenyl-4H-quinazolin-3-yl)phenoxy]- acetic acid [1-substituted aminomethyl-2-oxo-1,2-dihydro-indol-3-ylidene]- hydrazide derivatives and their potential biological activity
Havaldar, Freddy H.,Patil, Abhay R.
, p. 107 - 114 (2008/09/20)
[4-(4-Oxo-2-phenyl-4H-quinazolin-3-yl)-phenoxy]-acetic acid [2-oxo-1,2-dihydro-indol-3-ylidene]-hydrazide (7) on reaction with formaldehyde and various secondary amines in N,N-dimethyl formamide afforded Mannich bases [4-(4-oxo-2-phenyl-4H-quinazolin-3-yl
Synthesis, characterization and antiviral activity of 2,3-disubstituted quinazolones
Pandey,Kumar, Jitendra,Saxena,Mukesh,Joshi,Bajpai
, p. 593 - 597 (2008/09/21)
Anthranilic acid on reaction with excess equivalent of an aromatic acid chloride in pyridine yields 2-aryl-4-oxo-3,1-benzoxazines (1). Reaction of 1 with p-aminophenol in pyridine furnishes 2-aryl-3-(4-hydroxyphenyl)-4-oxo(3if)- quinazolones (2) which rea
Efficient solid phase synthesis of diverse quinazolinones
Makino,Suzuki,Nakanishi,Tsuji
, p. 1670 - 1672 (2007/10/03)
Various quinazolinones were synthesized by cyclocondensation of anthranilamides with a variety of orthoformates on solid supports. Alkyl, aryl and alkoxy groups can substitute at 2 position of quinazolines with this method. The reactions proceeded smoothly under mild acidic conditions and the products exhibited excellent purity. Unlike previously reported solid phase quinazolinone syntheses, this synthetic strategy does not require an oxidation step. The approach is applicable to the synthesis of a wide range of quinazolinones, including molecules that are susceptible to oxidation.
Synthesis of 6,8-Disubstituted 3-(4-)-2-phenylquinazolin-4(3H)-ones as Possible Antibacterial Agents
Sengupta, A. K.,Gupta, M. M.,Gupta, Anurag Ateet
, p. 600 - 602 (2007/10/02)
Several 6,8-disubstituted 3-(4-)-2-phenylquinazolin-4(3H)-ones (IIIa-o) have been synthesised by the reaction of 6,8-disubstituted 3-(4-hydroxyphenyl)-2-phenylquinazolin-4(3H)-ones (II) with N-chloroacetyl-N'-arylureas and evaluated for their antibacterial activity against Staph. aureus Bacillus pumillus, B. cereus and B. substilis.
