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Takahisa Imamura, Yoji Murakami, Hidetoshi Nitta
No abstract available.
April 21, 2017: Biological Chemistry
Yuanbiao Tu, Caolin Wang, Shan Xu, Zhou Lan, Wei Li, Jiaqian Han, Yuanzhang Zhou, Pengwu Zheng, Wufu Zhu
Two series of quinazoline derivatives bearing aryl semicarbazone scaffolds (9a-o and 10a-o) were designed, synthesized and evaluated for the IC50 values against four cancer cell lines (A549, HepG2, MCF-7 and PC-3). The selected compound 9o was further evaluated for the inhibitory activity against EGFR kinases. Four of the compounds showed excellent cytotoxicity activity and selectivity with the IC50 values in single-digit μM to nanomole range. Two of them are equal to more active than positive control afatinib against one or more cell lines...
April 6, 2017: Bioorganic & Medicinal Chemistry
Dong Young Kim, Jisu Kang, Song Eun Lee, Young Kwan Kim, Seung Soo Yoon
Two blue emitters based on fluorene-bridged quinazoline and quinoxaline derivatives were prepared via the Suzuki reaction. Their photoluminescent properties were investigated. Furthermore, theoretical studies on these materials using the density functional theory calculation were conducted. To explore their electroluminescent properties, multilayered organic light-emitting diodes were fabricated with the following device structure: indium-tin-oxide (180 nm)/4,4'-bis(N-(1-naphthyl)-N-phenylamino)biphenyl (50 nm)/blue emitting materials (1 and 2) (30 nm)/bathophenanthroline (35 nm)/8-hydroxy-quinolinato lithium (2 nm)/Al (100 nm)...
April 19, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
Jianquan Liu, Yong-Gang Ma, Mei-Mei Zhang, Xiang-Shan Wang
consecutive Sonogashira coupling reaction, acetylene hydroamination cyclization of 2-(2-bromophenyl)quinazolin-4(3H)-ones and terminal alkynes is described catalyzed by CuI/L-proline in the presence of Cs2CO3. This procedure provided a facile method for the synthesis of isoindolo[1,2-b]quinazolin-10(12H)-one derivatives in good yields.
April 19, 2017: Journal of Organic Chemistry
Prashantha Gunaga, John L Lloyd, Somanadham Mummadi, Abhisek Banerjee, Naveen Kumar Dhondi, James K Hennan, Veena Subray, Ramya Jayaram, Nagendra Rajugowda, Umamaheshwar Reddy, Duraimurugan Kumaraguru, Umasankar Mandal, Dasthagiri Beldona, Ashok Kumar Adisechan, Navnath Yadav, Jayakumar Warrier, James A Johnson, Harinath Sale, Siva Prasad Putlur, Ajay Saxena, Anjaneya Chimalakonda, Sandhya Mandlekar, Mary Lee Conder, Dezhi Xing, Arun Kumar Gupta, Anuradha Gupta, Richard A Rampulla, Arvind Mathur, Paul C Levesque, Ruth R Wexler, Heather J Finlay
We have recently disclosed 5-phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine 1 as a potent IKur current blocker with selectivity versus hERG, Na and Ca channels and an acceptable preclinical PK profile. On further characterization in vivo, Compound 1 demonstrated an unacceptable level of brain penetration. In an effort to reduce the level of brain penetration while maintaining the overall profile, SAR was developed at the C2' position for a series of close analogs by employing hydrogen bond donors...
April 18, 2017: Journal of Medicinal Chemistry
Kayleigh L Brocklesby, Jennifer S Waby, Chris Cawthorne, Graham Smith
Vandetanib is an orally available tyrosine kinase inhibitor used in the treatment of cancer. The current synthesis proceeds via an unstable 4-chloroquinazoline, using harsh reagents, in addition to requiring sequential protection and deprotection steps. In the present work, use of the Dimroth rearrangement in the key quinazoline forming step enabled the synthesis of Vandetanib in nine steps (compared to the previously reported 12-14).
April 12, 2017: Tetrahedron Letters
Saligrama Devegowda Preethi, Balaji Kyathegowdanadoddi Srinivas, Prasanna Doddakunche Shivaramu, Swaroop Toreshettahally Ramesh, Shankar Jayarama, Rangappa KanchKanchugarakoppal Subbegowda, Lokesh Siddalingaiah Gowda
A series of novel 4-anilino-6,7-dimethoxy quinazoline derivatives were synthesized and characterized using 1H, 13C NMR and FT-IR and mass spectroscopic techniques. Cytotoxicity assays were performed for all compounds against different cell lines such as human colon carcinoma (HCT116), human chronic myeloid leukemia (K562) and human breast cancer (SKBR3) cell lines using 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT), Tryphan blue and Lactose dehydrogenase release assay. Among all compounds, RB4, RB7 showed moderate activity whereas RB1 showed most potent activity comparable with that of the standard drug cisplatin against all three cells lines...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
Chao Yu, Xuefeng Guo, Zheng Xi, Michelle Muzzio, Zhouyang Yin, Bo Shen, Junrui Li, Christopher Seto, Shouheng Sun
We report a seed-mediated growth of 2.3 nm AgPd nanoparticles (NPs) in the presence of 40 × 5 nm WO2.72 nanorods (NRs) for the synthesis of AgPd/WO2.72 composites. The strong interactions between AgPd NPs and WO2.72 NRs make the composites, especially the Ag48Pd52/WO2.72, catalytically active for dehydrogenation of formic acid (TOF = 1718 h-1 and Ea = 31 kJ/mol), and one-pot reactions of formic acid, 2-nitrophenol and aldehydes into benzoxazoles in near quantitative yields under mild conditions. The catalysis can also be extended to the one-pot reactions of ammonium formate, 2-nitroacetophenone and aldehyde for high yield syntheses of quinazolines...
April 12, 2017: Journal of the American Chemical Society
Shakhinur Islam Mondal, Zabed Mahmud, Montasir Elahi, Arzuba Akter, Nurnabi Azad Jewel, Md Muzahidul Islam, Sabiha Ferdous, Taisei Kikuchi
Protein-protein interaction (PPI) and host-pathogen interactions (HPI) proteomic analysis has been successfully practiced for potential drug target identification in pathogenic infections. In this research, we attempted to identify new drug target based on PPI and HPI computation approaches and subsequently design new drug against devastating enterohemorrhagic Escherichia coli O104:H4 C277-11 (Broad), which causes life-threatening food borne disease outbreak in Germany and other countries in Europe in 2011...
December 2016: In Silico Pharmacology
Shenghai Guo, Jianhui Zhai, Fang Wang, Xuesen Fan
A practical and highly efficient procedure for the selective preparation of 6,6a-dihydroisoindolo[2,1-a]quinazoline-5,11-diones through a palladium-catalyzed one-pot three-component cascade reaction of 2-aminobenzamides with 2-bromobenzaldehydes and carbon monoxide under atmospheric pressure has been developed. This cascade reaction, in which four new C-C/C-N bonds and two new rings are simultaneously constructed, is triggered by a cyclocondensation of 2-aminobenzamides with 2-bromobenzaldehydes, followed by a Pd-catalyzed cyclocarbonylation of the in situ formed 2,3-dihydroquinazolin-4(1H)-ones with CO (1 atm)...
April 11, 2017: Organic & Biomolecular Chemistry
Hassanein H Hassanein, Hanan H Georgey, Marwa A Fouad, Ahmed M El Kerdawy, Mona F Said
AIM: The discovery of new generation of selective COX-2 inhibitors with potential analgesic and anti-inflammatory activity and minimal side effects is a major interest. MATERIALS & METHODS: Novel imidazole and imidazo[1,5-a]quinazoline derivatives were prepared and evaluated for their analgesic and anti-inflammatory activities. COX-1/COX-2 isozyme selectivity testing and molecular docking were performed. Key physicochemical parameters were calculated. RESULTS: All tested compounds exhibited significant activities compared with indomethacin as reference drug...
April 10, 2017: Future Medicinal Chemistry
Murat Bozdag, Ahmed Mahmoud Alafeefy, Abdul Malik Altamimi, Fabrizio Carta, Claudiu T Supuran, Daniela Vullo
We report a series of novel metanilamide-based derivatives 3a-q bearing the 2-mercapto-4-oxo-4H-quinazolin-3-yl moiety as tail. All compounds were synthesized by means of straightforward condensation procedures and were investigated in vitro for their inhibition potency against the human (h) carbonic anhydrase (CA; EC isoforms I, II, IX and XII. Among all compounds tested the 6-iodo 3g and the 7-fluoro 3i derivatives were the most potent inhibitors against the tumor associated CA IX and XII isoform (KIs 1...
May 15, 2017: Bioorganic & Medicinal Chemistry
Takumi Abe, Koshiro Kida, Koji Yamada
We have developed a copper-catalyzed Ritter-type reaction/cyclization cascade of anthranilic acids and nitriles, affording the quinazolin-4(3H)-ones. The cascade proceeds through a Ritter-type reaction capturing the iminoketene intermediates by nitriles. Furthermore, we found a novel Ritter-type reaction/condensation/intramolecular anti-Markovnikov hydroamination cascade, providing access to functionalized diazocines in one-pot.
April 4, 2017: Chemical Communications: Chem Comm
David Xu, Liwei Li, Donghui Zhou, Degang Liu, Andy Hudmon, Samy O Meroueh
Target-specific scoring methods are more commonly used to identify small-molecule inhibitors among compounds docked to a target of interest. Top candidates that emerge from these methods have rarely been tested for activity and specificity across a family of proteins. In this study we docked a chemical library into CaMKIIδ, a member of the Ca(2+) /calmodulin (CaM)-dependent protein kinase (CaMK) family, and re-scored the resulting protein-compound structures using Support Vector Machine SPecific (SVMSP), a target-specific method that we developed previously...
March 29, 2017: ChemMedChem
Mudassier Ahmad, Mushtaq A Aga, Javeed Ahmad Bhat, Brijesh Kumar, Abdul Rouf, Neena Capalash, Mubashir Javeed Mintoo, Ashok Kumar, Priya Mahajan, Dilip Manikrao Mondhe, Amit Nargotra, Parduman Raj Sharma, Mohmmad Afzal Zargar, Ram A Vishwakarma, Bhahwal Ali Shah, Subhash Chandra Taneja, Abid Hamid
l-Vasicine is a quinazoline alkaloid with an electron dense ring and additional functionalities in its structure. Employing target oriented synthesis (TOS) based on in silico studies, molecules with significant docking scores containing different derivatives of l-vasicine as caps were synthesized. Interestingly, one molecule, i.e., 4a, which contained 3-hyroxypyrrolidine as a cap group and a six carbon long aliphatic chain as a linker was found to inhibit HDACs. 4a showed more specificity toward class I HDAC isoforms...
April 13, 2017: Journal of Medicinal Chemistry
Takayuki Kosaka, Junko Tanizaki, Raymond Paranal, Hideki Endoh, Christine Lydon, Marzia Capelletti, Claire E Repellin, Jihyun Choi, Atsuko Ogino, Antonio Calles, Dalia Ercan, Amanda Redig, Magda Bahcall, Geoffrey R Oxnard, Michael Eck, Pasi A Janne
Insertion mutations in EGFR and HER2 both occur at analogous positions in exon 20. Non-small cell lung cancer (NSCLC) patients with tumors harboring these mutations seldom achieve clinical responses to dacomitinib and afatinib, two covalent quinazoline-based inhibitors of EGFR or HER2, respectively. In this study, we investigated the effects of specific EGFR and HER2 exon 20 insertion mutations from NSCLC patients that had clinically achieved a partial response after dacomitinib treatment. We identified Gly770 as a common feature among the drug-sensitive mutations...
March 31, 2017: Cancer Research
Hui Luo, Shengjie Yang, Da Hong, Wei Xue, Pu Xie
BACKGROUND: Cancer is one of the leading causes of death and only second to heart diseases. Recently, preclinical studies have demonstrated that curcumin had a number of anticancer properties. Thus, we planned to synthesize a series of curcumin analogs to assess their antiproliferation efficacy. RESULTS: A series of (1E,4E)-1-aryl-5-(2-((quinazolin-4-yl)oxy)phenyl)-1,4-pentadien-3-one derivatives (curcumin analogs) were synthesized and characterized by IR, NMR, and elemental analysis techniques...
2017: Chemistry Central Journal
Marwa F Ahmed, Radwan El-Haggar
New 6,8-dibromo-2-(4-chlorophenyl)-quinazoline-sulphonamide hybrids and some Schiff´s base analogs were synthesized, and their structures were confirmed by spectral and elemental analysis. Cytotoxicity of all synthesized compounds was evaluated on three cancer cell lines MCF7, HCT116 and HEPG2 using sulpharodamine-B assay method and doxorubicin as a reference drug. All tested compounds show promising cytotoxic activities on the three cell lines. Compound IXd was 2 times more active than doxorubicin on MCF7 cancer cells, while it was 3 times more potent than doxorubicin on HCT116 cancer cells...
March 27, 2017: Anti-cancer Agents in Medicinal Chemistry
Mostafa M Ghorab, Mohamed S A El-Gaby, Mansour S Alsaid, Yaseen A M M Elshaier, Aiten M Soliman, Fardous F El-Senduny, Farid A Badria
A series of novel thioureas 5a-n, 8, quinazoline 6, benzo[g]quinazoline 7 and benzo[1,3] dioxole 10, bearing a sulfonamide moiety were synthesized from the starting compound N-(2,6-dimethoxypyrimidin-4-yl)-4-isothiocyanatobenzenesulfonamide 2. The target compounds were screened against HepG2, MCF-7, Caco-2, HCT-116, PC-3 cancer cell lines and VERO-B normal cell line. Out of all the tested compounds, compound 5c showed a broad selective cytotoxicity against HepG2, MCF-7, Caco-2 and PC-3 cancer cells. Moreover, a sensitization assay was performed on Caco-2 cells, compound 5c proved to act as a chemosensitizer for cisplatin on colon cancer (Caco-2) cells...
March 27, 2017: Anti-cancer Agents in Medicinal Chemistry
Qianqian Qiu, Baomin Liu, Jian Cui, Zheng Li, Xin Deng, Hao Qiang, Jieming Li, Chen Liao, Bo Zhang, Wei Shi, Miaobo Pan, Wenlong Huang, Hai Qian
P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a principal obstacle for successful cancer chemotherapy. A novel P-gp inhibitor with a quinazoline scaffold, 12k, was considered to be the most promising for in-depth study. 12k possessed high potency (EC50 = 57.9 ± 3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells. 12k also boosted the potency of other MDR-related cytotoxic agents with different structures, increased accumulation of DOX, blocked P-gp-mediated Rh123 efflux, and suppressed P-gp ATPase activity in K562/A02 MDR cells...
April 5, 2017: Journal of Medicinal Chemistry
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