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Quinazoline

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https://www.readbyqxmd.com/read/28210215/tryptanthrin-suppresses-the-activation-of-the-lps-treated-bv2-microglial-cell-line-via-nrf2-ho-1-antioxidant-signaling
#1
Young-Won Kwon, So Yeong Cheon, Sung Yun Park, Juhyun Song, Ju-Hee Lee
Microglia are the resident macrophages in the central nervous system (CNS) and play essential roles in neuronal homeostasis and neuroinflammatory pathologies. Recently, microglia have been shown to contribute decisively to neuropathologic processes after ischemic stroke. Furthermore, natural compounds have been reported to attenuate inflammation and pathologies associated with neuroinflammation. Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione) is a phytoalkaloid with known anti-inflammatory effects in cells...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28177550/synthesis-anticonvulsant-activity-and-sar-study-of-novel-4-quinazolinone-derivatives
#2
Nada A Noureldin, Hend Kothayer, El-Sayed M Lashine, Mohamed M Baraka, Wafaa El-Eraky, Sally A El Awdan
Series of N-(4-substitutedphenyl)-4-(1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkanamides (5a-j) and 4-chloro-N'-((1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkaloyl)benzohydrazides (6a-f) were designed based on the previously reported essential structural features for anticonvulsant activity. Several amino acids were incorporated within the synthesized quinazolin-4(3H)-ones to improve their bioavailability and the anticonvulsant activity. Synthesis of the target compounds was accomplished in four steps starting from the reaction between N-methyl isatoic anhydride and the appropriate amino acid...
February 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28173708/synthesis-and-in-vitro-anti-proliferative-activity-of-some-novel-isatins-conjugated-with-quinazoline-phthalazine-hydrazines-against-triple-negative-breast-cancer-mda-mb-231-cells-as-apoptosis-inducing-agents
#3
Wagdy M Eldehna, Hadia Almahli, Ghada H Al-Ansary, Hazem A Ghabbour, Mohamed H Aly, Omnia E Ismael, Abdullah Al-Dhfyan, Hatem A Abdel-Aziz
Treatment of patients with triple-negative breast cancer (TNBC) is challenging due to the absence of well- defined molecular targets and the heterogeneity of such disease. In our endeavor to develop potent isatin-based anti-proliferative agents, we utilized the hybrid-pharmacophore approach to synthesize three series of novel isatin-based hybrids 5a-h, 10a-h and 13a-c, with the prime goal of developing potent anti-proliferative agents toward TNBC MDA-MB-231 cell line. In particular, compounds 5e and 10g were the most active hybrids against MDA-MB-231 cells (IC50 = 12...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28168646/synthesis-of-lactones-and-other-heterocycles
#4
REVIEW
Xi Liu, Liang-Nian He
Chemical fixation of CO2 into value-added chemicals represents a promising field in view of sustainable development and green synthesis. In this aspect, the construction of heterocyclic compounds from CO2 and readily available starting materials is particularly appealing in both organic and pharmaceutical fields since CO2 can be regarded as carbon and oxygen resource with advantages of abundance, renewability, non-toxicity, and non-flammability. In this chapter, we have summarized elegant protocols with elaborately designed substrates for the direct incorporation of entire CO2 molecule or "CO" or "C" fragments into lactones and other heterocycles such as oxazolidinones, cyclic carbonates, quinazoline-2,4(1H,3H)-diones, etc...
April 2017: Topics in Current Chemistry (Journal)
https://www.readbyqxmd.com/read/28166995/design-synthesis-and-anticancer-properties-of-isocombretaquinolines-as-potent-tubulin-assembly-inhibitors
#5
Ilhem Khelifi, Timothée Naret, Dolor Renko, Abdallah Hamze, Guillaume Bernadat, Jérome Bignon, Christine Lenoir, Joëlle Dubois, Jean-Daniel Brion, Olivier Provot, Mouad Alami
The synthesis and evaluation of a new series of IsoCombretaQuinolines (IsoCoQuines) 2 with a 2-substituted-quinoline in place of the 3,4,5-trimethoxyphenyl ring present in isoCA-4 and CA-4 are described. Most of these compounds displayed a potent cytotoxic activity (IC50 < 10 nM) against a panel of five human cancer cell lines and inhibited tubulin assembly at a micromolar level. The most potent analogue 2b, having a 3-hydroxy-4-methoxyphenyl as B-ring, led to cell cycle arrest in G2/M phase. Docking studies indicate that 2b showed a binding mode comparable to those previously observed with quinazoline analogous (IsoCoQ) and with isoCA-4 at the colchicine binding site of tubulin...
February 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28133651/acetic-acid-promoted-cascade-n-acyliminium-ion-aza-prins-cyclization-stereoselective-synthesis-of-functionalized-fused-tricyclic-piperidines
#6
Rajiv T Sawant, Marc Y Stevens, Luke R Odell
A novel acetic acid-promoted metal-free cascade N-acyliminium ion/aza-Prins cyclization of o-formyl carbamates and homoallylamines is reported. This one-pot protocol provides efficient and rapid access to masked cis-hydroxyhexahydropyrido[1,2-c]quinazolin-6-ones with concomitant generation of two stereogenic centers, four C-C/C-O/C-N bonds and two new rings in good yield and excellent diastereoselectivity.
February 9, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28125041/synthesis-modelling-and-anticonvulsant-studies-of-new-quinazolines-showing-three-highly-active-compounds-with-low-toxicity-and-high-affinity-to-the-gaba-a-receptor
#7
Mohamed F Zayed, Saleh K Ihmaid, Hany E A Ahmed, Khaled El-Adl, Ahmed M Asiri, Abdelsattar M Omar
Some novel fluorinated quinazolines (5a-j) were designed and synthesized to be evaluated for their anticonvulsant activity and their neurotoxicity. Structures of all newly synthesized compounds were confirmed by their infrared (IR), mass spectrometry (MS) spectra, ¹H nuclear magnetic resonance (NMR), (13)C-NMR, and elemental analysis (CHN). The anticonvulsant activity was evaluated by a subcutaneous pentylenetetrazole (scPTZ) test and maximal electroshock (MES)-induced seizure test, while neurotoxicity was evaluated by a rotorod test...
January 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28110817/quinazolinone-derivatives-synthesis-and-comparison-of-inhibitory-mechanisms-on-%C3%AE-glucosidase
#8
Mankun Wei, Wei-Ming Chai, Rui Wang, Qin Yang, Zhihong Deng, Yiyuan Peng
In this study, eight quinazolinone derivatives were designed and synthesized. Their inhibitory activities on α-glucosidase were assessed in vitro. Two compounds: 2-(4-chlorophenyl)-quinazolin-4(3H)-one (CQ) and 2-(4-bromophenyl)-quinazolin-4(3H)-one (BQ) were found to be potent inhibitors of α-glucosidase with IC50 values of 12.5±0.1μM and 15.6±0.2μM, respectively. Spectroscopy methods were performed to analyze the inhibitory mechanisms of both compounds on α-glucosidase. The results revealed that they reversibly inhibited α-glucosidase in a non-competitive manner...
September 17, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28093794/design-synthesis-and-biological-evaluation-of-novel-quinazoline-clubbed-thiazoline-derivatives
#9
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
#10
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
#11
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
#12
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 Subroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs
Novel antimalarial therapeutics that target multiple stages of the parasite 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 comparable to the known antimalarials, chloroquine and mefloquine...
February 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28074949/new-compounds-from-a-hydrothermal-vent-crab-associated-fungus-aspergillus-versicolor-xz-4
#13
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...
February 1, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28069069/arresting-kinase-suppressor-of-ras-in-an-inactive-state
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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