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Quinazoline

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https://www.readbyqxmd.com/read/28093794/design-synthesis-and-biological-evaluation-of-novel-quinazoline-clubbed-thiazoline-derivatives
#1
Zulphikar Ali, Md J Akhtar, Anees A Siddiqui, Ahsan A Khan, Md R Haider, Mohammad S Yar
A novel series of quinazoline clubbed thiazoline derivatives was rationally designed and synthesized. The newly synthesized compounds were evaluated for in vitro dipeptidyl peptidase IV (DPP-4) inhibitory activity. Compounds that showed good to moderate activity were compared using linagliptin as standard. Compound 4x (IC50  = 1.12 nM) exhibited the most promising results. The special chemical feature of compound 4x also imparts good inhibition selectivity for DPP-4 over DPP-8/9. Moreover, docking of compound 4x into the active site of DPP-4 illustrates its possible binding interactions...
January 17, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28092860/design-synthesis-and-biological-evaluation-of-quinazoline-phosphoramidate-mustard-conjugates-as-anticancer-drugs
#2
Songwen Lin, Yingbo Li, Yufen Zheng, Laichun Luo, Qi Sun, Zemei Ge, Tieming Cheng, Runtao Li
A series of novel compounds with phosphoramide mustard functionality incorporated into the quinazoline scaffold of EGFR/HER2 inhibitors were designed and synthesized as multi-target-directed ligands against tumor cells. In vitro assays showed that tumor cell lines with high HER2 level were more sensitive to the compounds than tumor cells with low HER2 level. Compound 10d (EMB-3) was one of the most potent inhibitors with IC50 of 7.4 nM and 82 nM against EGFR and HER2, respectively. The mechanism studies were also supported by the effect of 10d-induced DNA damage in MDA-MB-468 cells...
January 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28087274/study-of-antileishmanial-activity-of-2-aminobenzoyl-amino-acid-hydrazides-and-their-quinazoline-derivatives
#3
Sherine Nabil Khattab, Nesreen Saied Haiba, Ahmed Mosaad Asal, Adnan A Bekhit, Aida A Guemei, Adel Amer, Ayman El-Faham
A new small library of 2-aminobenzoyl amino acid hydrazide derivatives and quinazolinones derivatives was synthesized and fully characterized by IR, NMR, and elemental analysis. The activity of the prepared compounds on the growth of Leishmania aethiopica promastigotes was evaluated. 2-Benzoyl amino acid hydrazide showed higher inhibitory effect than the quinazoline counterpart. The in vitro antipromastigote activity demonstrated that compounds 2a, 2b, 2f and 4a had IC50 better than standard drug miltefosine and comparable activity to amphotericin B deoxycholate, which indicates their high antileishmanial activity against Leishmania...
January 5, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28080063/optimization-of-2-anilino-4-amino-substituted-quinazolines-into-potent-antimalarial-agents-with-oral-in-vivo-activity
#4
Paul R Gilson, Cyrus Tan, Kate E Jarman, Kym N Lowes, Joan M Curtis, William Nguyen, Adrian E Di Rago, Hayley E Bullen, Boris Prinz, Sandra Duffy, Jonathan B Baell, Craig A Hutton, Helene Jousset Sabroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs
Novel antimalarial therapeutics that target multiple stages of the parasites lifecycle are urgently required to tackle the emerging problem of resistance with current drugs. Here we describe the optimization of the 2-anilino quinazoline class as antimalarial agents. The class, identified from publicly available antimalarial screening data, was optimized to generate lead compounds that possess potent antimalarial activity against P. falciparum parasites equivalent to the known antimalarials, chloroquine and mefloquine...
January 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28074949/new-compounds-from-a-hydrothermal-vent-crab-associated-fungus-aspergillus-versicolor-xz-4
#5
Chengqian Pan, Yutong Shi, Xuegang Chen, Chen-Tung Arthur Chen, Xinyi Tao, Bin Wu
Three new quinazoline derivatives (1-3), one new oxepin-containing natural product (4) and four new cyclopenin derivatives (5-7 and 9) have been isolated from an EtOAc extract of the Taiwan Kueishantao hydrothermal vent crab-associated fungus Aspergillus versicolor XZ-4. Their planar structures were established by HRMS, 1D and 2D NMR spectroscopic data analyses. The absolute configurations for compounds 1 and 4 were determined by chiral phase HPLC analysis of their hydrolysis products. The absolute configurations of 2, 3 and 7 were defined mainly by comparison of the quantum chemical TDDFT calculated and the experimental ECD spectra, and the absolute configuration of 5 was deduced from comparison of the optical rotation values reported in the literature...
January 11, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28069069/arresting-kinase-suppressor-of-ras-in-an-inactive-state
#6
EDITORIAL
Syed Lal Badshah, Yahia Mabkhot
Ras protein signaling pathways are important in controlling the plight of different types of cancer. Here we discussed the paper entitled "Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling" published in Nature journal on inactivating the kinase suppressor of Ras (KSR) protein using a small molecule as an inhibitor by Dhawan et al. A biphenyl ether analogue of a quinazoline binds in one of the binding pockets of KSR and results in stabilization of its inactive state...
January 9, 2017: Chinese Journal of Cancer
https://www.readbyqxmd.com/read/28063784/new-n-and-o-arylpiperazinylalkyl-pyrimidines-and-2-methylquinazolines-derivatives-as-5-ht7-and-5-ht1a-receptor-ligands-synthesis-structure-activity-relationships-and-molecular-modeling-studies
#7
Sebastiano Intagliata, Maria N Modica, Valeria Pittalà, Loredana Salerno, Maria A Siracusa, Alfredo Cagnotto, Mario Salmona, Rafał Kurczab, Giuseppe Romeo
Based on our earlier studies of structure activity relationships on 4-substituted piperazine derivatives, in this work we synthesized a novel set of long-chain arylpiperazines with the purpose of elucidating if some structural modifications in the terminal fragment could affect the binding affinity for the 5-HT7 and 5-HT1A receptors. In this new series, the quinazolinone system of the previous derivatives was replaced by a 6-phenylpyrimidine or a 2-methylquinazoline, which were used as versatile building blocks for the preparation of new compounds...
December 27, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28059042/alkaloids-as-cyclooxygenase-inhibitors-in-anticancer-drug-discovery
#8
Muhammad Ali Hashmi, Afsar Khan, Umar Farooq, Sehroon Khan
Cancer is the leading cause of death worldwide and anticancer drug discovery is a very hot area of research at present. There are various factors which control and affect cancer, out of which enzymes like cyclooxygenase-2 (COX-2) play a vital role in the growth of tumor cells. Inhibition of this enzyme is a very useful target for the prevention of various types of cancers. Alkaloids are a diverse group of naturally occurring compounds which have shown great COX-2 inhibitory activity both in vitro and in vivo...
January 5, 2017: Current Protein & Peptide Science
https://www.readbyqxmd.com/read/28056730/synthesis-molecular-docking-and-evaluation-of-3-4-2-amino-4-substitutedphenyl-2h-1-3-oxazin-thiazin-6-yl-2-phenyl-3h-quinazolin-4-one-derivatives-for-their-anticonvulsant-activity
#9
Nimisha Jain, Jugnu Jaiswal, Ashish Pathak, Pradeep Kumar Singour
BACKGROUND: According to World Health Organization (WHO), around 50 million people worldwide suffering from epilepsy. Therefore, continued search for safer and more effective anticonvulsants is urgently necessary. OBJECTIVES: The present work was to synthesize 2-phenyl substituted quiazolinone derivatives and to evaluate them for anticonvulsant activity and neurotoxic. METHODS: A series of novel 3-{4-[2-amino-4-(substitutedphenyl)-2H-[1.3] oxazin/thiazin-6-yl} 2-phenyl-3H-quinazolin-4-one derivatives were synthesized and evaluated for their anticonvulsant activity...
January 4, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28044161/a-concise-construction-of-12h-benzo-4-5-thiazolo-2-3-b-quinazolin-12-ones-via-an-unusual-tbhp-na2co3-promoted-cascade-oxidative-cyclization-and-interrupted-dimroth-rearrangement
#10
Zhi-Wen Zhou, Feng-Cheng Jia, Cheng Xu, Shi-Fen Jiang, Yan-Dong Wu, An-Xin Wu
An efficient transition-metal-free cascade reaction has been developed for the facile synthesis of 12H-benzo[4,5]thiazolo[2,3-b]quinazolin-12-one derivatives from commercially available isatins and 2-haloaryl isothiocyanates. A preliminary mechanistic study suggested an interrupted Dimroth rearrangement was the key step for the successful transformation.
January 3, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28042842/novel-2-3-dihydro-1h-pyrrolo-3-2-1-ij-quinazolin-1-ones-synthesis-and-biological-evaluation
#11
Malose J Mphahlele, Tebogo A Khoza, Peaceful Mabeta
Herein we describe the synthesis and evaluation of a series of novel 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinazolin-1-ones for in vitro cytotoxicity against three human cancer cell lines as well as for potential antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum. The title compounds were prepared via PdCl₂-mediated endo-dig cyclization of 2-aryl-8-(arylethynyl)-6-bromo-2,3-dihydroquinazolin-4(1H)-ones. The latter were prepared, in turn, via initial Sonogashira cross-coupling of 2-amino-5-bromo-3-iodobenzamide with aryl acetylenes followed by boric acid-mediated cyclocondensation of the intermediate 2-amino-3-(arylethynyl)-5-bromobenzamides with benzaldehyde derivatives...
December 30, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28039712/egfr-inhibition-studies-by-hybrid-scaffolds-for-their-activity-against-ovarian-cancer
#12
Feng Zhang, Hongyan Zhang, Fang Wang
PURPOSE: A series of quinazoline isatine hybrid derivatives were designed and their molecular docking studies were performed to ascertain the inhibition of EGFR by these hybrids. METHODS: Molecular modelling and docking methods were employed to design and synthesize the molecules. The compounds which showed good binding properties were synthesized and characterized. After structural confirmation of these compounds they were evaluated for their antiproliferative activity on OVCAR-3 ovarian cancer cell line...
November 2016: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/28011211/2-guanidino-quinazolines-as-a-novel-class-of-translation-inhibitors
#13
E S Komarova Andreyanova, I A Osterman, P I Pletnev, Y A Ivanenkov, A G Majouga, A A Bogdanov, P V Sergiev
A variety of structurally unrelated organic compounds has been reported to have antibacterial activity. Among these, certain small-molecule translation inhibitors have attracted a great deal of attention, due to their relatively high selectivity against prokaryotes, and an appropriate therapeutic index with minor "off target" effects. However, ribosomes are being considered as poorly druggable biological targets, thereby making some routine computational-based approaches to rational drug design and its development rather ineffective...
December 20, 2016: Biochimie
https://www.readbyqxmd.com/read/28010062/covalent-modulators-of-the-vacuolar-atpase
#14
Ying-Chu Chen, Keriann M Backus, Maria Merkulova, Christina Yang, Dennis Brown, Benjamin F Cravatt, Chao Zhang
The vacuolar H(+) ATPase (V-ATPase) is a complex multisubunit machine that regulates important cellular processes through controlling acidity of intracellular compartments in eukaryotes. Existing small-molecule modulators of V-ATPase either are restricted to targeting one membranous subunit of V-ATPase or have poorly understood mechanisms of action. Small molecules with novel and defined mechanisms of inhibition are thus needed to functionally characterize V-ATPase and to fully evaluate the therapeutic relevance of V-ATPase in human diseases...
January 18, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28002962/correction-to-2-3-methoxyphenyl-quinazoline-derivatives-a-new-class-of-direct-constitutive-androstane-receptor-car-agonists
#15
Tomas Smutny, Alice Nova, Marcela Drechslerová, Alejandro Carazo, Lucie Hyrsova, Zuzana Rania Hrušková, Jiří Kuneš, Milan Pour, Marcel Špulák, Petr Pavek
No abstract text is available yet for this article.
December 22, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28002645/biologically-active-heterocyclic-hybrids-based-on-quinazolinone-benzofuran-and-imidazolium-moieties-synthesis-characterization-cytotoxic-and-antibacterial-evaluation
#16
Parvin Asadi, Ghadamali Khodarahmi, Ali Jahanian-Najafabadi, Lotfollah Saghaie, Farshid Hassanzadeh
Cytotoxic and antimicrobial agents structurally based on quinazolinone, benzofuran and imidazole pharmacophores, have been designed and synthesized. Spectral (IR, (1) H NMR) and elemental analysis data established the structures of these novel 1-[[(1-(benzofuran-2-yl)-2-(quinazolin-4(3H)-one-3-yl)]ethyl-1-yl]-3- methyl imidazol-1-ium chloride hybrid derivatives. All the synthesized compounds were evaluated for in vitro cytotoxicity and antimicrobial activities. Cytotoxic evaluation using MTT assay revealed that compounds 12c, 12g and 12i exhibited significant cytotoxicity with IC50 values 1, 1, 0...
December 21, 2016: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28000898/regorafenib-induces-extrinsic-and-intrinsic-apoptosis-through-inhibition-of-erk-nf-%C3%AE%C2%BAb-activation-in-hepatocellular-carcinoma-cells
#17
Jai-Jen Tsai, Po-Jung Pan, Fei-Ting Hsu
The aim of the present study was to investigate the role of NF-κB inactivation in regorafenib-induced apoptosis in human hepatocellular carcinoma SK-HEP-1 cells. SK-HEP-1 cells were treated with different concentrations of the NF-κB inhibitor 4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine (QNZ) or regorafenib for different periods. The effects of QNZ and regorafenib on cell viability, expression of NF-κB-modulated anti-apoptotic proteins and apoptotic pathways were analyzed by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, western blotting, DNA gel electrophoresis, flow cytometry and NF-κB reporter gene assay...
February 2017: Oncology Reports
https://www.readbyqxmd.com/read/27994738/sulfonamides-as-selective-nav1-7-inhibitors-optimizing-potency-and-pharmacokinetics-to-enable-in-vivo-target-engagement
#18
Isaac E Marx, Thomas A Dineen, Jessica Able, Christiane Bode, Howard Bregman, Margaret Chu-Moyer, Erin F DiMauro, Bingfan Du, Robert S Foti, Robert T Fremeau, Hua Gao, Hakan Gunaydin, Brian E Hall, Liyue Huang, Thomas Kornecook, Charles R Kreiman, Daniel S La, Joseph Ligutti, Min-Hwa Jasmine Lin, Dong Liu, Jeff S McDermott, Bryan D Moyer, Emily A Peterson, Jonathan T Roberts, Paul Rose, Jean Wang, Beth D Youngblood, Violeta Yu, Matthew M Weiss
Human genetic evidence has identified the voltage-gated sodium channel NaV1.7 as an attractive target for the treatment of pain. We initially identified naphthalene sulfonamide 3 as a potent and selective inhibitor of NaV1.7. Optimization to reduce biliary clearance by balancing hydrophilicity and hydrophobicity (Log D) while maintaining NaV1.7 potency led to the identification of quinazoline 16 (AM-2099). Compound 16 demonstrated a favorable pharmacokinetic profile in rat and dog and demonstrated dose-dependent reduction of histamine-induced scratching bouts in a mouse behavioral model following oral dosing...
December 8, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27994726/quinazoline-carboxamides-as-selective-antagonists-of-adenosine-2a-receptor
#19
EDITORIAL
Gerard Rosse
No abstract text is available yet for this article.
December 8, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27988418/supercritical-water-oxidation-of-quinazoline-reaction-kinetics-and%C3%A2-modeling
#20
Yanmeng Gong, Yang Guo, Shuzhong Wang, Wenhan Song, Donghai Xu
This paper presents a first quantitative kinetic model for supercritical water oxidation (SCWO) of quinazoline that describes the formation and interconversion of intermediates and final products at 673-873 K. The set of 11 reaction pathways for phenol, pyrimidine, naphthalene, NH3, etc, involved in the simplified reaction network proved sufficient for fitting the experimental results satisfactorily. We validated the model prediction ability on CO2 yields at initial quinazoline loading not used in the parameter estimation...
December 11, 2016: Water Research
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