- Design and synthesis of potent N-phenylpyrimidine derivatives for the treatment of skin cancer
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The development of novel synthetic compounds for the treatment of skin cancer is much needed, as there is a sudden rise in the incidence of skin cancer throughout the world and the available chemotherapy is facing problems of resistance. Hence, present re
- Chaube, Udit J.,Vyas, Vivek K.,Bhatt, Hardik G.
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- Bacterial cell leakage potential of newly synthesized quinazoline derivatives of 1,5-benzodiazepines analogue
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Novel quinazoline embellished analogues of 1,5-benzodiazepine (6, 9, 13, 17, 21 and 24) were synthesized using one-pot domino approach. Structure of the compounds synthesized, were established with the help of IR, 1H NMR, 13C NMR and
- Dwivedi, Jaya,Kishore, Dharma,Misra, Apoorva,Sharma, Swapnil,Shukla, Shruti
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- Synthesis and bioactivity of 2-cyanoacrylates containing a trifluoromethylphenyl moiety
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A series of 2-cyanoacrylates containing a trifluoromethylphenyl moiety were synthesized in three steps: ethyl 2-cyano-3,3-dimethylthioacrylate was prepared from ethyl cyanoacetate with carbon disulfide and dimethyl sulfate, then its reaction with 4-trifluoromethylaniline yielded ethyl 2-cyano-3-(4- trifluoromethylphenylamino)-3-methylthioacrylate, and then reacted with an alkylamine. The new structures were verified by elemental analysis, IR, 1H NMR and mass spectra. In the MTT test, these new compounds were found to possess high antitumor activities against PC3 and A431 cells.
- Song, Baoan,Yang, Song,Zhong, Huimin,Jin, Linhong,Hu, Deyu,Liu, Gang
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- Synthesis and biological evaluation of some 5-ethoxycarbonyl-6-isopropylamino-4-(substitutedphenyl)aminopyrimidines as potent analgesic and anti-inflammatory agents
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Synthesis and biological evaluation of some 5-ethoxycarbonyl-6-isopropylamino-4-(substitutedphenyl)aminopyrimidines have been achieved by cyclization of N-[2-ethoxycarbonyl-2-cyano-1-(isopropylamino)vinyl] formamidine in presence of dry HCl in dioxane fol
- Chhabria, Mahesh T.,Bhatt, Hardik G.,Raval, Hitesh G.,Oza, Pratik M.
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- Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors
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N,N′-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene aminal-based lactam derivatives as potent and orally active FXa inhibitors.
- Shi, Yan,Zhang, Jing,Stein, Philip D.,Shi, Mengxiao,O'Connor, Stephen P.,Bisaha, Sharon N.,Li, Chi,Atwal, Karnail S.,Bisacchi, Gregory S.,Sitkoff, Doree,Pudzianowski, Andrew T.,Liu, Eddie C.,Hartl, Karen S.,Seiler, Steven M.,Youssef, Sonia,Steinbacher, Thomas E.,Schumacher, William A.,Rendina, Alan R.,Bozarth, Jeffrey M.,Peterson, Tara L.,Zhang, Ge,Zahler, Robert
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- A sensitive and highly selective fluorescent sensor for In3+
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A simple neutral fluorescent sensor based on pyrazolo[1,5-a]pyrimidine exhibited a unique selectivity for indium(iii) ion (In3+) over various other metal ions with dramatic fluorescence response in acetonitrile. The Royal Society of Chemistry 2
- Wu, Yan-Chao,Li, Hui-Jing,Yang, Hua-Zheng
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- Synthesis, antiviral and antifungal bioactivity of 2-cyano-acrylate derivatives containing phosphonyl moieties
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Alkyl 2-cyano-3-methylthio-3-phosphonylacrylates were synthesized by the reaction of alkyl 2-cyano-3,3-dimethylthioacrylates with dialkyl phosphites. The structures of the new compounds were characterized by elemental analyses, IR, 1H-, 13
- Lv, Yin-Pu,Wang, Xian-You,Song, Bao-An,Yang, Song,Yan, Kai,Xu, Guang-Fang,Bhadury, Pinaki S.,Liu, Fang,Jin, Lin-Hong,Hu, De-Yu
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- A Metal-Free Approach for the Synthesis of 2-Tetralones via Carbanion-Induced Ring Transformation of 2 H -Pyran-2-ones
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A metal-free, ultrasound-assisted approach for the synthesis of highly functionalized 2-tetralones in high yields is described. The process involves ring transformation of 2 H -pyran-2-ones with the spirocyclic ketone 1,4-cyclohexandione monoethylene keta
- Shetgaonkar, Samata E.,Singh, Fateh V.
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- Synthesis, spectral characterization and photophysical studies of tetrahydroquinolines
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A metal-free, ultrasound-assisted, fast synthesis of fluorescent N-Boc-protected 1,2,3,4–tetrahydroquinolines 9a-p is described through carbanion-induced ring transformation of 6-aryl-2H-pyran-2-ones 7 with tert?butyl 3-oxopiperidine-1-carboxylate 8 under
- Kennedy, L. John,Singh, Fateh V.,Subashini, C.
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- Design, synthesis and biological evaluation of novel DPP-IV inhibitors
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Diabetes mellitus is one of the top ten leading causes of death worldwide. DPP-IV inhibition became an attractive target in controlling type 2 diabetes. Because of the several adverse effects associated with current DPP-IV inhibitors, the discovery and de
- Karelia, Chirag,Parmar, Kailash,Teli, Divya,Chhabria, Mahesh
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p. 1227 - 1235
(2020/12/04)
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- Tailored-design Synthesis of Sulfapyrimidine Derivatives
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In this paper, we report an efficient and convenient approach for the synthesis of tailored-design target sulfapyrimidine derivatives expected to show remarkable antimicrobial activities. The approach is based on reacting arylsulfonyl guanidine with α,β-unsaturated carbonyl compounds to afford N-(4,6-diarylpyrimidin-2-yl)arylsulfonamide or with ylidene derivatives to afford N-(6-aryl-5-cyanopyrimidin-2-yl)arylsulfonamide, N-(4-amino-5-cyano-6-(methylthio)-pyrimidin-2-yl)-arylsulfonamide, and N-(5-cyanopyrimidin-2-yl)arylsulfonamide compounds through Michael addition reaction. The structure of the newly synthesized compounds was confirmed from spectral data and elemental analysis.
- Azzam, Rasha A.
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p. 619 - 627
(2019/01/04)
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- Microwave assisted base dependent regioselective synthesis of partially reduced chromenes, isochromenes and phenanthrenes
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We have reported a microwave assisted base directed regioselective synthesis of partially reduced chromenes, isochromenes and phenanthrenes. Functionalized 4-(piperidin-1-yl)-5,6-dihydro-2H-benzo[h]-chromen-2-one-3- carbonitriles have been used as precurs
- Yadav, Pratik,Singh, Surjeet,Sahu, Satya Narayan,Hussain, Firasat,Pratap, Ramendra
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p. 2228 - 2234
(2014/04/03)
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- PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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New pyrrolotriazinone derivatives having the chemical structure of formula (I), are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
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(2014/05/07)
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- Synthesis of some novel α-cyanoketene-n, s-acetals derived from secondary aliphatic amines and their use in pyrazole synthesis
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New α-cyanoketene-N,S-acetals 2(a-g) and β-dialkylamine-α- cyanoacrylates 3(g-i) were synthesized in good to excellent yields by the reaction of ethyl 2-cyano-3, 3-bis(methylthio)acrylate 1 with secondary aliphatic amines (i.e., N-methylalkyl- and N-ethyl
- Al-Adiwish, Wedad M.,Tahir,Yaacob
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supporting information
p. 3203 - 3216
(2014/01/06)
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- Design, microwave-assisted synthesis and in silico docking studies of new 4H-pyrimido[2,1-b]benzothiazole-2-arylamino-3-cyano-4-ones as possible adenosine A2B receptor antagonists
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A series of new 4H-pyrimido[2,1-b]benzothiazole-2-arylamino-3-cyano-4-ones 6a-g have been designed and synthesized by the application of microwave-assisted organic synthesis (MAOS) technique. In silico docking studies have been carried out to gain an insi
- Balakumar,Kishore, D. Pran,Rao, K. Venkat,Narayana, B. Lakshmi,Rajwinder,Rajkumar,Rao, A. Raghuram
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p. 1105 - 1113
(2012/11/13)
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- Synthesis and pharmacological investigation of 5-substituted-3- methylsulfanyl-1 H-pyrazole-4-carboxylic acid ethyl esters as new analgesic and anti-inflammatory agents
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Purpose: To synthesize a new series of 5-substituted-3-methylsulfanyl-1H- pyrazole-4-carboxylic acid ethyl esters for their analgesic and anti-inflammatory activity. Methods: The title compound synthesized by reacting the amino group of 5-amino-3-methylsu
- Gokulan,Jayakar,Alagarsamy,Raja Solomon
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p. 457 - 462
(2013/01/15)
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- 1H-PYRAZOLO [3, 4-B] PYRIDINE COMPOUNDS FOR INHIBITING RAF KINASE
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Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. [FORMULA I]
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Page/Page column 53
(2011/04/14)
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- RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
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Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment
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Page/Page column 56
(2011/04/14)
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- Synthesis and biological evaluation of pyrido(2, 3-d)pyrimidine-carboxylate derivatives
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Ethyl-5-amino-8-(4-halophenyl)-2-methyl-4,7-dioxo-3,4,5,6,7,8-hexahydro pyrido(2,3-d) pyrimidine-6-carboxylate and ethyl-5-amino-8-(4-halophenyl)-2- amino-4,7 dioxo-3,4,5,6,7,8 hexahydropyrido(2,3-d)pyrimidine-6-carboxylate derivatives have been synthesiz
- Shanmugasundaram,Harikrishnan,Vijey Aanandini,Sathish, Kumar M.,Sateesh
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experimental part
p. 284 - 289
(2011/05/02)
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- Synthesis and antiviral bioactivities of 2-cyano-3-substitutedamino(phenyl) methylphosphonylacrylates (Acrylamides) containing alkoxyethyl moieties
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An efficient reaction under microwave irradiation has been developed for the synthesis of a series of novel 2-cyano-3-substituted-amino(phenyl) methylphosphonylacrylates (acrylamides) II. The products obtained in shorter reaction time with moderate yields are fully characterized by elemental analysis, IR, 1H, 13C, and 31P NMR spectral data. The role of introducing various substituents and the effect of incorporating a-aminophosphonates with an alkoxyethyl moiety into the parent cyanoacrylate (acrylamide) structure are investigated. Among the studied compounds, both II-17 and II-24 displayed good in vivo curative, protection, and inactivation effects, which were comparable to those of the commercial reference ningnanmycin (inhibitory rates of 58.8, 60.2, 78.9% and 60.0, 58.9, 85.5%, respectively, at 500 mg/L against TMV). To the best of the authors' knowledge, this is the first report on the synthesis and antiviral activity of the title compounds II.
- Yang, Jia-Qiang,Song, Bao-An,Bhadury, Pinaki S.,Chen, Zhuo,Yang, Song,Xue-Jian, Cai,Hu, De-Yu,Xue, Wei
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p. 2730 - 2735
(2011/07/31)
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- PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS
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Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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(2009/10/22)
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- Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors
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Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This s
- Gopalsamy, Ariamala,Ciszewski, Greg,Shi, Mengxiao,Berger, Dan,Hu, Yongbo,Lee, Frederick,Feldberg, Larry,Frommer, Eileen,Kim, Steven,Collins, Karen,Wojciechowicz, Donald,Mallon, Robert
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scheme or table
p. 6890 - 6892
(2010/05/19)
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- Synthesis and antiviral activities of cyanoacrylate derivatives containing an α-aminophosphonate moiety
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Target compounds 8 were obtained by the reaction of alkyl 2-cyano-3,3-dimethylthioacrylate or cyarylamide (7a-7e) and α- aminobenzylphosphonate (5a-5e) under reflux condition using ethanol as solvent. Their structures were clearly verified by spectroscopic data (IR and 1H, 13C, and 31P NMR) and elemental analysis. These compounds were shown to be antivirally active in the bioassay. It was found that title compounds 8d and 8e had the same inactivation effect against tobacco mosaic virus (EC50 = 55.5 and 55.3 μg/mL) as the commercial product ningnanmycin (EC50 = 50.9 μg/mL). To the best of our knowledge, this is the first report on the synthesis and antiviral activity of cyanoacrylate derivatives containing an α-aminophosphonate moiety.
- Long, Ning,Cai, Xue-Jian,Song, Bao-An,Yang, Song,Chen, Zhuo,Bhadury, Pinaki S.,Hu, De-Yu,Jin, Lin-Hong,Xue, Wei
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scheme or table
p. 5242 - 5246
(2010/04/06)
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- Pyrazolo[1,5-A]pyrimidine derivatives and methods of use thereof
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The present invention relates to pyrazolo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a pyrazolo[1,5-a]pyrimidine derivative and methods for treating or preventing cancer, comprising administering to a subject in need thereof an effective amount of a pyrazolo[1,5-a]pyrimidine derivative.
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Page/Page column 34
(2010/11/28)
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- An easy access to variously substituted pyrroles starting from ketene dithioacetals
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Variously substituted pyrroles 4 can easily be synthesized in two steps by reacting a primary or secondary amine and a ketene dithioacetal in a basic medium in moderate to good yield. Ketene dithioacetals 2 are readily prepared from acetylaceton or malononitrile, carbon disulfide, and methyl iodide.
- Sommen, Geoffroy L.,Cornel, Alain,Kirsch, Gilbert
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p. 693 - 699
(2007/10/03)
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- Synthesis of 2-cyanoacrylates containing pyridinyl moiety under ultrasound irradiation
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Reaction of ethyl cyanoacetate with carbon disulfide and dimethyl sulfate in the presence of sodium methoxide in anhydrous methanol yields ethyl 2-cyano-3,3-dimethyl-thioacrylate, followed by the nucleophilic substitution with 2-amino-3-chloro-4- methylpy
- Zhang, Huiping,Song, Baoan,Zhong, Huimin,Yang, Song,Jin, Linhong,Hu, Deyu,He, Wei
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p. 1211 - 1214
(2007/10/03)
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- Synthesis of novel heterocyclic compounds: Routes to pyrazolyl 1,2,3-triazoles and their biological activity evaluation
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A series of 5-aryl-3-cyanomethylpyrazoles have been synthesized by refluxing 6-aryl-3-cyano-4-methylthio-2H-pyran2-ones with hydrazine. The active methylene moiety of these pyrazoles has further been exploited to build 1,4-disubstituted 5-amino-1,2,3-tria
- Kumar, Ajay,Husain, Mofazzal,Prasad, Ashok K.,Singh, Ishwar,Vats, Archana,Sharma, Nawal K.,Sharma, Sunil K.,Gupta, Rajinder K.,Olsend, Carl E.,Bracke, Marc E.,Gross, Richard A.,Parmar, Virinder S.
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p. 1950 - 1957
(2007/10/03)
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- Novel intramolecular cyclization of pyrazolone ketene S,N-acetals for the construction of methylsulfanylpyrazolo-[4,3-b]pyridines
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A novel and efficient method for the synthesis of 6-substituted-7,7a-dihydro-1,7a-dimethyl-7-imino-2-phenyl-1H-pyrazolo[4, 3-b]pyridin-3(2H)-ones via the reaction of 4-amino-2,3-dimethyl-1-phenylpyrazolin-5-one with ketene dithioacetals and ethoxy-methylenemalononitrile or ethyl ethoxymethylene-cyanoacetate followed by intramolecular cyclization of the products has been investigated.
- Elgemeie, Galal H.,Elzanate, Ali M.,Elghandour, Ahmed H.,Ahmed, Sayed A.
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p. 3509 - 3517
(2007/10/03)
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- Synthesis of E- and Z-Pyrazolylacrylonitriles and their evaluation as novel antioxidants
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A facile synthesis of (Z)- and (E)-2-(5-arylpyrazol-3-yl)-3-(pyrrol-2-yl)acrylonitriles and (Z)-2-(1,3-diarylpyrazol-5-yl)-3-(pyrrol-2-yl)acrylonitriles, and isomerisation of (Z)-2-(5-arylpyrazolyl)acrylonitriles to (E)-2-(5-arylpyrazolyl)acrylonitriles under basic conditions have been reported. (Z)-2-(1,3-Diarylpyrazolyl)acrylonitriles did not undergo isomerisation under the similar conditions. New compounds were identified on the basis of their spectral data (1H-, 13C-, 1H-1H COSY, NOESY, NOE, HMQC NMR, IR, UV and EI mass). The structures of one acrylonitrile and five of their precursor 6-arylpyran-2-ones and cyanomethylpyrazoles were confirmed by X-ray crystallographic studies. Effects of pyrazolylacrylonitriles and their precursors on rat liver-microsomal lipid peroxidation were evaluated in vitro with a view to establish structure-activity relationship and to identify a lead compound. Copyright (C) 1999 Elsevier Science Ltd.
- Parmar, Virinder S.,Kumar, Ajay,Prasad, Ashok K.,Singh, Sanjay K.,Kumar, Naresh,Mukherjee, Shubhasish,Raj, Hanumantharao G.,Goel, Sanjay,Errington, William,Puar, Mohindar S.
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p. 1425 - 1436
(2007/10/03)
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- SYNTHESIS OF SOME NEW FUSED HETEROCYCLES CONTAINING A BRIDGEHEAD NITROGEN ATOM UNDER PTC CONDITIONS. A NEW APPLICATION OF CYANOKETENE S,S-ACETALS
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A novel synthesis of some fused heterocyclic compounds containing a bridgehead nitrogen atom was achieved using PTC conditions.Suitable ketene S,S-acetals were thus prepared and allowed to react with some o-substituted anilines to give (2,3-dihydrobenzothiazol-2-ylidenyl)malonodinitrile, 2a, ethyl (2,3-dihydrobenzothiazol-2-ylidenyl)cyanoacetate, 2b, (2,3-dihydrobenzoxazol-2-ylidenyl)malonodinitrile, 2c, ethyl (2,3-dihydrobenzoxazol-2-ylidenyl)cyanoacetate, 2d, (2,3-dihydrobenzimidazol-2-ylidenyl)malonodinitrile, 2e, and ethyl (2,3-dihydrobenzimidazol-2-ylidenyl)cyanoacetate, 2f.These afforded the desired products on reaction with a variety of halo compounds.
- El-Shafei, Ahmed Kamal,Soliman, Ahmed Mohamed,Sultan, Adel Abdel-Rahim,El-Saghier, Ahmed Mohamed Mohamed
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p. 115 - 118
(2007/10/02)
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- Synthesis, Reactions, and Tautomerism of Ketene N,S-Acetals with Benzothiazoline Ring
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Ketene dithioacetals 2 react with 2-aminothiophenol to afford the corresponding substituted 2(3H)-methylenebenzothiazoles 3.Some compounds 3 react with α,β-unsaturated esters to give 1H-pyridobenzothiazole derivatives 4 and 5 by an electrophilic addition and cyclocondensation sequence.
- Huang, Zhi-Tang,Shi, Xian
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p. 541 - 547
(2007/10/02)
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- Heteroatom Rearrangements. S,N, O,N, and N,N Double Rearrangements. X-Ray Molecular Structure of 5-Cyano-6-methylthio-2,3-diphenyl-pyrimidin-4(3H)-one
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New heteroatom rearrengements are reported; 'S,N, O,N, and N,N double rearrangements' take place when acrylonitriles, substituted at C-3 by two heteroatom groups (MeS or MeSe, and SH, OH, or NHPh), condense with aromatic carboxylic acids in the presence o
- Yokoyama, Masataka,Hatanaka, Hidekatsu,Sasaki, Atsuhi,Shiraishi, Tadashi,Kumata, Katsushi,et al.
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p. 1187 - 1196
(2007/10/02)
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- Synthesis of 5,6-Dihydro-4H-1,3,5-dithiazines, 2,3-Dihydro-6-thioxo-6H-1,3-thiazine, and 6-Amino-1,3-dithiins
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Dithiolates (1) or (2), derived from compounds containing an active methylene or a sulphonamido-group, carbon disulphide and sodium or potassium hydroxide, underwent a Mannich reaction with formaldehyde and a primary amine to form 5,6-dihydro-1,3,5-dithiazines (3) or (4).The dithiolate (12), derived from ethyl acetoacetate, cyclised under the above conditions to ethyl 2,3-dihydro-3,4-dimethyl-6-thioxo-6H-1,3-thiazine-5-carboxylate (18).The dithiolates (20), derived from cyanoacetic ester, or (10), derived from acetophenone, interacted with formaldehyde and cyanoacetic esters or with 2-cyanoacrylates to form 6-amino-1,3-dithiins (26) or iminodithians (28).Methyl 6-amino-2--1,3-dithiin-5-carboxylate (26; R1=Et, R2=Me) formed N-acyl derivatives with aliphatic acid chlorides.On oxidation the dithiin (26; R1=Et, R2=Me) contracted to ethyl 2-cyano-2-(4-cyano-1,3-dithiolan-5-ylidene)acetate (31).
- Howes, P.D.,Payne, J.J.,Pianka, M.
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p. 1038 - 1044
(2007/10/02)
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