- Highly Chemoselective Deoxygenation of N-Heterocyclic N-Oxides Using Hantzsch Esters as Mild Reducing Agents
-
Herein, we disclose a highly chemoselective room-temperature deoxygenation method applicable to various functionalized N-heterocyclic N-oxides via visible light-mediated metallaphotoredox catalysis using Hantzsch esters as the sole stoichiometric reductant. Despite the feasibility of catalyst-free conditions, most of these deoxygenations can be completed within a few minutes using only a tiny amount of a catalyst. This technology also allows for multigram-scale reactions even with an extremely low catalyst loading of 0.01 mol %. The scope of this scalable and operationally convenient protocol encompasses a wide range of functional groups, such as amides, carbamates, esters, ketones, nitrile groups, nitro groups, and halogens, which provide access to the corresponding deoxygenated N-heterocycles in good to excellent yields (an average of an 86.8% yield for a total of 45 examples).
- An, Ju Hyeon,Kim, Kyu Dong,Lee, Jun Hee
-
supporting information
p. 2876 - 2894
(2021/02/01)
-
- Unsymmetrical bisquinolines with high potency against P. falciparum Malaria
-
Quinoline-based scaffolds have been the mainstay of antimalarial drugs, including many artemisinin combination therapies (ACTs), over the history ofmoderndrugdevelopment. Althoughmuch progress has beenmade in the search for novel antimalarial scaffolds, itmay be that quinolineswill remain useful, especially if very potent compounds fromthis class are discovered. We report here the results of a structure-activity relationship(SAR) study assessingpotentialunsymmetrical bisquinoline antiplasmodial drug candidates using in vitro activity against intact parasites in cell culture. Many unsymmetrical bisquinolineswere found to be highly potent against both chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum parasites. Further work to develop such compounds could focus on minimizing toxicities in order to find suitable candidates for clinical evaluation.
- Burgess, Steven J.,Gunsaru, Bornface,Kelly, Jane X.,Li, Yuexin,Liebman, Katherine M.,Liebman, Michael C.,Morrill, Westin,Peyton, David H.
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-
- QUINOLINE-BASED COMPOUNDS AND METHODS OF INHIBITING CDK8/19
-
Disclosed herein are quinoline-based compounds and method for inhibiting CDK8 or CDK19 for the intervention in diseases, disorders, and conditions. The quinoline-based composition comprise substituents at quinoline ring positions 4 and 6, wherein the substituent at position 4 is selected from a substituted or unsubstituted arylalkylamine or a substituted or unsubstituted arylhetrocyclylamine. Pharmaceutical compositions comprising the substituted qunioline compositions, methods of inhibiting CDK8 or CDK19, and methods of treating CDK8/19-associated diseases, disorders, or conditions are also disclosed.
- -
-
Paragraph 0108; 0117-0118; 0123
(2020/03/09)
-
- Synthesis and biological evaluations of N′-substituted methylene-4-(quinoline-4-amino) benzoylhydrazides as potential anti-hepatoma agents
-
In the effort to develop novel quinoline derivatives for the treatment of liver cancer, we synthesized a series of N′-Substituted methylene-4-(quinoline-4-amino) benzoylhydrazides and evaluated their biological activities as anticancer agents. Compounds 5
- Fang, Meijuan,He, Fengming,Huang, Qingqing,Li, Baicun,Liu, Xiaoguang,Qiu, Yingkun,Wu, Tong,Wu, Zhen,Xue, Yuhua,Zhao, Taige,Zhu, Feifeng
-
-
- Derivative containing aromatic ring/aromatic heterocycle-triazole-methylene-TCP and preparation method and application thereof
-
The invention discloses a derivative containing aromatic ring/aromatic heterocycle-triazole-methylene-TCP, which has a structure shown in a general formula I, has remarkable biological inhibition activity on LSD1, can be used for preparing a medicine for inhibiting LSD1, enriches the variety of TCP derivatives, and lays a foundation for researching and developing a novel LSD1 inhibitor. Particularly, the derivative can be used for preparing anti-tumor medicines, has a certain inhibition effect on a plurality of tumor cell strains such as gastric cancer cell strains (MGC-803, SGC-7901), breastcancer cell strains (MCF-7) and prostate cancer cell strains (PC-3), shows antitumor activity, provides a lead compound structure for anticancer drugs, and has a good application prospect. The invention also provides a preparation method of the aromatic ring/aromatic heterocycle-triazole-methylene-TCP containing derivative, (1R, 2S)-phenylcyclopropylamine or (1R, 2S)-3, 4-difluorophenylcyclopropylamine is used as a raw material, the derivative is prepared through alkyne feeding and cycloaddition reactions, the preparation method is simple, and batch production and commercial application are facilitated.
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-
Paragraph 0061; 0064
(2020/08/09)
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- Combining 1,3-Ditriazolylbenzene and Quinoline to Discover a New G-Quadruplex-Interactive Small Molecule Active against Cancer Stem-Like Cells
-
Quadruplex nucleic acids are promising targets for cancer therapy. In this study we used a fragment-based approach to create new flexible G-quadruplex (G4) DNA-interactive small molecules with good calculated oral drug-like properties, based on quinoline
- Mendes, Eduarda,Cadoni, Enrico,Carneiro, Filipa,Afonso, Marta B.,Brito, Hugo,Lavrado, Jo?o,dos Santos, Daniel J. V. A.,Vítor, Jorge B.,Neidle, Stephen,Rodrigues, Cecília M. P.,Paulo, Alexandra
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p. 1325 - 1328
(2019/06/21)
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- Synthesis and anti-gastric cancer activity evaluation of novel triazole nucleobase analogues containing steroidal/coumarin/quinoline moieties
-
A series of novel triazole nucleobase analogues containing steroidal/coumarin/quinoline moieties have been synthesized based on copper-catalyzed azide-alkyne cycloaddition (CuAAC). The anti-cancer activity of the new triazole nucleobase analogues was stud
- Zhao, Jian-Wei,Wu, Zeng-Hui,Guo, Jia-Wen,Huang, Ming-Jie,You, Ya-Zhen,Liu, Hong-Min,Huang, Li-Hua
-
supporting information
(2019/08/12)
-
- Design, synthesis, biological evaluation, and molecular modeling studies of quinoline-ferulic acid hybrids as cholinesterase inhibitors
-
A series of quinoline-ferulic acid hybrids has been designed, synthesized, and evaluated as cholinesterase inhibitors. Most of the compounds showed good inhibitory activities toward both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among them, 10f was found to be the most potent inhibitor against AChE (IC50 = 0.62 ± 0.17 μM), and 14 was the most potent inhibitor against BChE (IC50 = 0.10 ± 0.01 μM). Representative compounds, such as 10f and 12g, act in a competitive manner when they inhibit AChE or BChE. Molecular docking and dynamic simulation revealed that the synthesized compounds bind to the target by simultaneously interacting with the catalytic active site (CAS) and the peripheral anionic site (PAS) of both AChE and BChE. The U-shaped confirmation was preferred when 12g bound to BChE, which was different from the linear conformation of 10f bound to AChE. Cell-based assays have confirmed the moderate neuroprotective effects of compounds 10f and 12g against H2O2-induced oxidative damage towards PC12 cells. Moreover, the hepatotoxicity of 12g was lower than that of tacrine, indicating its potential safety as an anti-Alzheimer's agent. In summary, we report a new chemotype of multifunctional hybrid, which may be further modified to develop new anti-Alzheimer's agents.
- Mo, Jun,Yang, Hongyu,Chen, Tingkai,Li, Qihang,Lin, Hongzhi,Feng, Feng,Liu, Wenyuan,Qu, Wei,Guo, Qinglong,Chi, Heng,Chen, Yao,Sun, Haopeng
-
-
- 4-((2-substituted quinoline-4-yl)amino)benzoyl hydrazine derivatives as well as preparation method and application thereof
-
The invention relates to 4-((2-substituted quinoline-4-yl)amino)benzoyl hydrazine derivatives as well as a preparation method and application thereof, which relate to N'-substituted methylene-4-((2-substituted quinoline-4-yl)amino)benzoyl hydrazine deriva
- -
-
Paragraph 0047; 0049-0051
(2018/10/26)
-
- 1,4-disubstituted 1,2,3-triazole nucleoside analogues, and preparation method and application thereof
-
The invention belongs to the technical field of pharmaceutical chemistry, and relates to 1,4-disubstituted 1,2,3-triazole nucleoside analogues: design, synthesis and anti-gastric cancer activity research. The purine nucleoside analogues have the following
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-
Paragraph 0027; 0029-0030
(2018/09/08)
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- Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents
-
A series of novel 4-anilinoquinoline derivatives were synthesized and evaluated for their antiproliferative activities. Among them, 14h exhibited the most potent cytotoxic activity with IC50 values ranging from 1.5 to 3.9 nM against all tested cancer cell lines, and showed promising efficacy in multidrug resistant cancer cells. Flow cytometry assay, immune-fluorescence staining, microtubule dynamics assays and competition assays with EBI identified that 14h was a novel tubulin depolymerization agent by binding to the colchicine site. Importantly, in vivo efficacy evaluation of HCT116 xenograft model, 14h showed efficient antitumor activity without significant loss in body weight. All the results indicated that 14h could be a promising candidate for the treatment of cancer.
- Zhou, Yuanyuan,Yan, Wei,Cao, Dong,Shao, Mingfeng,Li, Dan,Wang, Fang,Yang, Zhuang,Chen, Yong,He, Linhong,Wang, Taijin,Shen, Mingsheng,Chen, Lijuan
-
supporting information
p. 1114 - 1125
(2017/08/02)
-
- TOLL-LIKE RECEPTOR 8 AGONISTS
-
Compounds described herein can be used for therapeutic purposes. The compounds can be TLR agonists, such as TLR8 agonists. The compounds can be included in pharmaceutical compositions and used for therapies were being a TLR8 agonist is useful. The pharmac
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Page/Page column 22; 23
(2015/07/07)
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- Iron(III)-mediated photocatalytic selective substitution of aryl bromine by chlorine with high chloride utilization efficiency
-
An iron(III)-mediated photocatalytic method for the conversion of aryl, heteroaryl and polycyclic aromatic bromides to the corresponding chlorides with high selectivity has been achieved successfully. The mild reaction conditions and high chloride utilization efficiency promise a bright future for chlorination reactions. The Royal Society of Chemistry 2014.
- Wang, Ying,Li, Lina,Ji, Hongwei,Ma, Wanhong,Chen, Chuncheng,Zhao, Jincai
-
supporting information
p. 2344 - 2346
(2014/03/21)
-
- Rhodium-catalyzed intramolecular hydroarylation of 1-halo-1-alkynes: Regioselective synthesis of semihydrogenated aromatic heterocycles
-
The regioselective intramolecular hydroarylation of (3-halo-2-propynyl) anilines, (3-halo-2-propynyl) aryl ethers, or (4-halo-3-butynyl) aryl ethers was efficiently catalyzed by Rh2(OCOCF3)4 to give semihydrogenated aromatic heterocycles, such as 4-halo-1,2-dihydroquinolines, 4-halo-3-chromenes, or 4-(halomethylene)chromans, in good to excellent yields. Some synthetic applications taking advantage of the halo-substituents of the products are also illustrated. Ring a rhodium! Regioselective intramolecular hydroarylation of haloacetylenes efficiently catalyzed by [Rh 2(tfa)4] (see scheme; tfa=OCOCF3) gave semihydrogenated aromatic heterocycles in good to excellent yields. Copyright
- Murase, Hirohiko,Senda, Kousuke,Senoo, Masato,Hata, Takeshi,Urabe, Hirokazu
-
supporting information
p. 317 - 322
(2014/01/17)
-
- A practical and mild chlorination of fused heterocyclic N-oxides
-
Fused azine N-oxides were selectively chlorinated at C2 in moderate to excellent yields, employing Vilsmeier reagent as both the activating agent and the nucleophilic chloride source. Remarkable features of the method include simple operation, mild reaction conditions, a wide substrate scope, and the use of only stoichiometric amount of POCl3. The potential extension of this method to a one-pot oxidation/chlorination sequence that obviates the need for isolation of the N-oxide intermediates is also validated.
- Wang, Dong,Jia, Hailing,Wang, Wuchang,Wang, Zhe
-
supporting information
p. 7130 - 7132
(2015/02/02)
-
- Chiral helical oligotriazoles: New class of anion-binding catalysts for the asymmetric dearomatization of electron-deficient N -heteroarenes
-
Helical chirality and selective anion-binding processes are key strategies used in nature to promote highly enantioselective chemical reactions. Although enormous efforts have been made to develop simple helical chiral systems and thus open new possibilities in asymmetric catalysis and synthesis, the efficient use of synthetic oligo- and polymeric helical chiral catalysts is still very challenging and rather unusual. In this work, structural unique chiral oligotriazoles have been developed as C-H bond-based anion-binding catalysts for the asymmetric dearomatization of N-heteroarenes. These rotational flexible catalysts adopt a reinforced chiral helical conformation upon binding to a chloride anion, allowing high levels of chirality transfer via a close chiral anion-pair complex with a preformed ionic substrate. This methodology offers a straightforward and potent entry to the synthesis of chiral (bioactive)heterocycles with added synthetic value from simple and abundant heteroarenes.
- Zurro, Mercedes,Asmus, S?ren,Beckendorf, Stephan,Mück-Lichtenfeld, Christian,Mancheo, Olga Garca
-
supporting information
p. 13999 - 14002
(2015/01/08)
-
- Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors
-
Inhibition of the VEGF signaling pathway has become a valuable approach in the treatment of cancers. In this work, a series of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives were designed and identified as potent inhibitors of VEGFR-2 (
- Shi, Lei,Wu, Ting-Ting,Wang, Zhi,Xue, Jia-Yu,Xu, Yun-Gen
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p. 698 - 707
(2014/08/18)
-
- Structure-based design of novel human toll-like receptor 8 agonists
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Toll-like receptor (TLR)-8 agonists activate adaptive immune responses by inducing robust production of T helper 1-polarizing cytokines, suggesting that TLR8-active compounds might be promising candidate vaccine adjuvants. Recently, a C2-butyl furo[2,3-c]
- Kokatla, Hari Prasad,Sil, Diptesh,Tanji, Hiromi,Ohto, Umeharu,Malladi, Subbalakshmi S.,Fox, Lauren M.,Shimizu, Toshiyoki,David, Sunil A.
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p. 719 - 723
(2014/05/06)
-
- Twisted cyanines: A non-planar fluorogenic dye with superior photostability and its use in a protein-based fluoromodule
-
The cyanine dye thiazole orange (TO) is a well-known fluorogenic stain for DNA and RNA, but this property precludes its use as an intracellular fluorescent probe for non-nucleic acid biomolecules. Further, as is the case with many cyanines, the dye suffer
- Shank, Nathaniel I.,Pham, Ha H.,Waggoner, Alan S.,Armitage, Bruce A.
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p. 242 - 251
(2013/02/25)
-
- BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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-
Paragraph 0328; 0329
(2013/08/28)
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- Synthesis of 4,5-bis(dimethylamino)quinolines and the dual direction of their protonation
-
A study on the synthesis of derivatives of 4,5-bis(dimethylamino)quinoline, which is a quinoline analog of 1,8-bis(dimethylamino)naphthalene (also known by its trade name Proton Sponge) was carried out. The first two representatives of this series were obtained. Depending on the aggregate state, solvent, and structural features, these compounds may be protonated either at the quinoline heteroatom or peri-NMe2 groups.
- Shmoilova,Dyablo,Pozharskii
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p. 1308 - 1322
(2014/01/17)
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- Phosphonium chloride as a non-volatile chlorinating reagent: Preparation and reaction in no solvent or ionic liquid
-
Reaction of triphenylphosphine with trichloroisocyanuric acid in no solvent or an ionic liquid gave the corresponding phosphonium chloride, which can be used as a cheap and safe chlorinating reagent. Conversion of hydroxyheterocycles to chloroheterocycles, carboxylic acids to carboxylic acid chlorides, and primary amides to nitriles were accomplished by using the phosphonium chloride in excellent to good yields.
- Sugimoto, Osamu,Harada, Yukihiro,Tanji, Ken-Ichi
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p. 1583 - 1590
(2013/08/15)
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- Novel Sulfonaminoquinoline Hepcidin Antagonists
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The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
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Page/Page column 172
(2012/09/05)
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- Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl) ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: Potent in vivo activity in Parkinson's disease anima
-
Here we report structure - activity relationship study of a novel hybrid series of compounds where structural alteration of aromatic hydrophobic moieties connected to the piperazine ring and bioisosteric replacement of the aromatic tetralin moieties were
- Ghosh, Balaram,Antonio, Tamara,Zhen, Juan,Kharkar, Prashant,Reith, Maarten E. A.,Dutta, Aloke K.
-
experimental part
p. 1023 - 1037
(2010/08/06)
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- Assembly of 4-aminoquinolines via palladium catalysis: A mild and convenient alternative to SNAr methodology
-
4-Aminoquinolines, classically prepared via SNAr chemistry from an amine and 4-haloquinoline, are important scaffolds in medicinal chemistry. Interest in these compounds prompted us to explore palladium catalysis as an alternative to the existing methods for their preparation. Initial results followed by an iterative screening paradigm confirmed Pd(OAc)2/ DPEphos/K3PO4 as a mild and convenient alternative for the formation of the C-N bond in 4-aminoquinolines. A description of the screen and the scope of this methodology are discussed herein.
- Margolis, Brandon J.,Long, Kimberly A.,Laird, Dana L. T.,Ruble, J. Craig,Pulley, Shon R.
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p. 2232 - 2235
(2007/10/03)
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- Solvent-free reaction using phosphonium salts: Chlorination of hydroxyheteroaromatics and dehydration of primary amides
-
Solvent-free chlorination of heteroaromatics using the phosphonium salt, prepared by reaction of triphenylphosphine with N-chlorosuccinimide, was accomplished by microwave-irradiation or heating to give the corresponding chloroheteroaromatics. Similarly, primary amides was converted into nitriles by this method.{A figure is presented}.
- Takahashi, Tatsuya,Sugimoto, Osamu,Koshio, Jiro,Tanji, Ken-ichi
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p. 1973 - 1979
(2007/10/03)
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- An efficient and general method for the deoxygenation of organic N-oxides using Zn(OTf)2 and Cu(OTf)2
-
A mild and efficient general method for the deoxygenation of organic N-oxides such as azoxybenzenes, N-arylnitrones, and N-heteroarene N-oxides using Zn(OTf)2 and Cu(OTf)2 in excellent yields is described. Georg Thieme Verlag Stuttgart.
- Saini, Anil,Kumar, Sanjay,Sandhu, Jagir S.
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p. 395 - 398
(2007/10/03)
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- Synthesis of n-chloroquinolines and n-ethynylquinolines (n=2, 4, 8): Homo and heterocoupling reactions
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The n-(ethynyl)quinolines were satisfactorily prepared by heterocoupling reaction between the appropriate n-chloroquinoline and 2-methyl-3-butyn-2-ol, catalyzed by palladium, followed by treatment with a catalytic amount of powdered sodium hydroxide in toluene. The n-(ethynyl)quinolines were transformed in the corresponding conjugate 1,4-bis[n′-(quinolyl)]buta-1,3-diynes by oxidative dimerization, catalyzed by cuprous chloride, with excellent yields. Moreover, the heterocoupling between n′-haloquinoline and n′-(ethynyl)quinoline (n′, 2′ or 3′), catalyzed by palladium, gives 2′,2′-bis(quinoline) or 1,2-di(3′-quinolyl) ethyne, respectively. The same coupling reaction with zerovalent nickel complexes, gives a mixture of 1,2,4- and 1,3,5-tri(n′-quinolyl)benzene.
- Rodríguez, J. Gonzalo,De Los Rios, Cristobal,Lafuente, Antonio
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p. 9042 - 9051
(2007/10/03)
-
- A general method for the deoxygenation of aromatic N-oxides using RuCl 3?xH2O
-
An efficient, simple and selective method for the deoxygenation of aromatic N-oxides, such as N-arylnitrones, azoxybenzenes, N-heteroarene N-oxides using ruthenium(III) chloride to afford deoxygenated products in excellent yields, is described.
- Kumar, Sanjay,Saini, Anil,Sandhu, Jagir S.
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p. 8737 - 8739
(2007/10/03)
-
- Aminopiperidine quinolines and their azaisosteric analogues with antibacterical activity
-
Aminopiperidine derivatives of formula (I) and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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-
-
- NITRO AND AMINO SUBSTITUTED TOPOISOMERASE AGENTS
-
The invention provides compounds of formula 1 : wherein R1-R9, W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula 1, processes for preparing compounds of formula 1, intermediates useful for preparing compounds of formula 1, and therapeutic methods for treating cancer using compounds of formula 1.
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-
-
- Nitro and amino substitution within the A-ring of 5H-8,9-dimethoxy-5-(2-N, N-dimethylaminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: Influence on topoisomerase I-targeting activity and cytotoxicity
-
Recently, 5H-8,9-dimethoxy-5-(2-N,N-dimethylaminoethyl)-2,3- methylenedioxydibenzo[c,h][1,6]naphthyridin-6-one, 1, was identified as a TOP1-targeting agent with pronounced antitumor activity. In the present study, the effect on activity of substituting a
- Ruchelman, Alexander L.,Kerrigan, John E.,Li, Tsai-Kun,Zhou, Nai,Liu, Angela,Liu, Leroy F.,LaVoie, Edmond J.
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p. 3731 - 3742
(2007/10/03)
-
- Discovery of quinazolines as a novel structural class of potent inhibitors of NF-κB activation
-
We disclose here a new structural class of low-molecular-weight inhibitors of NF-κB activation that were designed and synthesized by starting from quinazoline derivative 6a. Structure-activity relationship (SAR) studies based on 6a elucidated the structural requirements essential for the inhibitory activity toward NF-κB transcriptional activation, and led to the identification of the 6-amino-4-phenethylaminoquinazoline skeleton as the basic framework. In this series of compounds, 11q, containing the 4-phenoxyphenethyl moiety at the C(4)-position, showed strong inhibitory effects on both NF-κB transcriptional activation and TNF-α production. Furthermore, 11q exhibited an anti-inflammatory effect on carrageenin-induced paw edema in rats.
- Tobe, Masanori,Isobe, Yoshiaki,Tomizawa, Hideyuki,Nagasaki, Takahiro,Takahashi, Hirotada,Fukazawa, Tominaga,Hayashi, Hideya
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p. 383 - 391
(2007/10/03)
-
- IMPROVED PROCESS FOR THE PREPARATION OF HALO-4-PHENOXYQUINOLINES
-
The present invention relates to a new improved, simplified process for the preparation of halo-4-phenoxyquinolines, whereby thionyl chloride is used as the chlorinating agent to prepare the corresponding chloroquinoline intermediate prior to the final co
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-
-
- Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
-
Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
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-
-
- An indium mediated efficient chemoselective deoxygenation of N-oxides and nitrones
-
A simple and inexpensive procedure for the deoxygenation of N-oxides, such as N-arylnitrones, azoxybenzenes and N-heteroarene N-oxides with indium trichloride in acetonitrile at ambient pressure is described. The procedure gives high yields of deoxygenated products.
- Ilias, Md,Barman, Dhiren C,Prajapati, Dipak,Sandhu, Jagir S
-
p. 1877 - 1879
(2007/10/03)
-
- Syntheses and photochromic behavior of biquinolinium salts
-
Three isomers of N,N′-dibenzy-biquinolinium dibromide were synthesized and their photoinduced coloration properties were investigated in the thin poly(N-vinylpyrrolidone) films. Upon photo-irradiation, the colorless film of 4,4′-biquinolinium salt became
- Nanasawa,Tomoda,Hirai
-
p. 163 - 168
(2007/10/03)
-
- A novel one-pot synthesis of 4-chloro-3-quinolinecarboxaldehydes, 4-chloroquinolines and 4-chloro-3-ethylquinolines using Vilsmeier reagent
-
Various substituted l-(2-aminophenyl)ethanones on treatment with Vilsmeier reagent at 90°C for 3-6 hr yield 4-chloro-3-quinolinecarboxaldehydes. Whereas substituted N-[2-(1- oxoethyl) phenyl] acetamides afford both 4-chloroqui-nolines and 4-chloro-3-quinolinecarboxaldehydes. However, in the case of substituted l-(2-aminophenyl)butanones and N-[2(1-oxopropyl) phenyl] acetamides, only 4-chloro-3-ethylquinolines are obtained.
- Amaresh,Perumal
-
p. 541 - 544
(2007/10/03)
-
- An Efficient General Method for the Deoxygenation of N-Arylnitrones, Azoxybenzenes, and N-Heteroarene N-Oxides
-
A new general method for the deoxygenation of N-oxides such as N-arylnitrones, azoxybenzenes, and N-heteroarene N-oxides uses aluminum iodide in acetonitrile.The deoxygenated products are obtained in high yields.
- Konwar, Dilip,Boruah, Romesh C.,Sandhu, Jagir S.
-
p. 337 - 339
(2007/10/02)
-
- PHOTODECARBOXYLATIVE CHLORINATION OF CARBOXYLIC ACIDS VIA THEIR BENZOPHENONE OXIME ESTERS
-
Decarboxylative chlorination of various aromatic and aliphatic carboxylic acids is performed successfully by the photolysis of their benzophenone oxime esters in carbon tetrachloride and corresponding chloro compounds are prepared in good yields.High selective generation of the certain radical and efficiency of the stable radical precursor, benzophenone oxime ester, afford much advantage for radical chemistry.
- Hasebe, Masato,Tsuchiya, Takashi
-
p. 6287 - 6290
(2007/10/02)
-
- Synthesis of 7,8,9,10-tetrahydropyrido[3',4':4,5]pyrrolo[2,3-c]quinolines
-
A series of structurally novel 7,8,9,10-tetrahydropyrido [3',4':4,5]pyrrolo[2,3-c]quinolines, 4a-c, were synthesized via a facile Fischer indole cyclization from the appropriately substituted hydrazinoquinolines 2a-c. Acetamides 4a,c were hydrolyzed to 5a
- Schonafinger,Yasenchak,Vollman,Ong
-
p. 535 - 537
(2007/10/02)
-
- Titanium(0) Reagents; 2. A Selective and Efficient Deoxygenation of Halogen Containing Heteroaromatic N-Oxides
-
Following successful reductions of unfunctionalized heteroaromatic N-oxides by titanium(0), we applied this method to halogenated aromatic N-oxides to give the deoxygenated halogeno derivatives in 90-95percent yield.
- Malinowski, Marek,Kaczmarek, Lukasz
-
p. 1013 - 1015
(2007/10/02)
-
- Substituent effects in the hydrolysis of quinoline-boranes
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Rates of hydrolysis of quinoline-boranes (QB) in aqueous dioxane are dramatically influenced by substitution in both the hetero and all-carbon ring systems. Effects of 3-, 4-, and 6-substituents appear to be due to electronic induction. Rates obtained at 25 °C with 3- and 4-substituted quinoline-boranes correlate with Hammett σm and σp parameters for both acid-independent and acid-catalyzed pathways, which are depicted respectively by k1 and k2 in the expression -d[QB]/dt = [QB](k1 + k2[H+]). Results are consistent with previously proposed mechanisms involving, for the first-order process, dissociative loss of BH3 and, for the acid-catalyzed reaction, electrophilic displacement of BH3 via cis attack of hydrogen ion at nitrogen. Methyl substitution at C-2 enhances k1 presumably through a steric effect and k2 through an inductive effect. A significant steric effect of the peri hydrogen at C-8 is suggested through a comparison of kinetic parameters for substituted quinoline-boranes with those of isoquinoline-borane, wherein k1 may be observed to change by over 4 orders of magnitude. Such substituent effects are significant in the projected synthetic use of heteroaromatic amine-boranes in protic media.
- Minter, David E.,Kelly, Curtis R.,Kelly, Henry C.
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p. 3291 - 3294
(2008/10/08)
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- 4-Piperidino-2-phenylquinolines
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Disclosed are compounds of the formula STR1 wherein: R1 and R2 may be either the same or different and each is hydrogen or lower alkyl; and wherein R3 and R4 may be either the same or different and each is hydrogen, halogen, or lower alkyl, with the proviso that R3 and R4 cannot both be hydrogen. These compounds are useful as anticonvulsant or anxiolytic agents.
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