- Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma
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No new and effective treatments have been approved for the treatment of esophageal squamous cell carcinoma (ESCC) in the past decade. Cisplatin and 5-fluoruracil are the most commonly used drugs for this disease. In order to develop a new class of drugs effective in our ESCC phenotypic screens, we began a systematic approach to generate novel compounds based on the 2-oxo-1,2-dihydroquinoline-4-carboxamide fragment. Herein, we report on the synthesis and initial assessment of 55 new analogues in two ESCC cell lines. Some of the active analogues with IC50 values around 10 μM were tested in three additional cell lines. Our structure-activity relationships revealed remarkable alterations in the anti proliferative activities upon modest chemical modifications and autophagy modulation is a suggested mechanism of action.
- Shahin, Mai I.,Roy, Joyeeta,Hanafi, Maha,Wang, Dongyao,Luesakul, Urarika,Chai, Yifeng,Muangsin, Nongnuj,Lasheen, Deena S.,Abou El Ella, Dalal A.,Abouzid, Khaled A.,Neamati, Nouri
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p. 516 - 530
(2018/06/15)
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- Novel synthesis of 4-or 6-substituted indirubin derivatives
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A simple and convenient route for synthesis of a series of 4-or 6-substituted indirubin derivatives by oxidation and subsequent condensation of indoxyl and isatin is described. Acidic reaction conditions are crucial to the condensation of 4-substituted derivatives, whereas for the condensation of 6-substituted derivatives, both acidic and basic conditions work well. Copyright Taylor & Francis Group, LLC.
- Zhang, Aiying,Yu, Mingfeng,Lan, Tian,Liu, Zenglu,Mao, Zhenmin
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experimental part
p. 3125 - 3134
(2010/12/24)
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- Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors
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A series of N-benzylated isatin oximes were developed as inhibitors of the mitogen-activated kinase, JNK3. X-ray crystallographic structures aided in the design and synthesis of novel, selective compounds, that inhibit JNK3, but not p38 MAP kinase and provided key insights into understanding the behavior of gatekeeper residue methionine-146 in determining target selectivity for this series.
- Cao, Jingrong,Gao, Huai,Bemis, Guy,Salituro, Francesco,Ledeboer, Mark,Harrington, Edmund,Wilke, Susanne,Taslimi, Paul,Pazhanisamy,Xie, Xiaoling,Jacobs, Marc,Green, Jeremy
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scheme or table
p. 2891 - 2895
(2010/01/16)
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- Catalytic enantioselective fluorination of oxindoles
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We have developed a highly efficient catalytic enantioselective fluorination of oxindole derivatives. In the presence of a catalytic amount of chiral Pd complex 2 (2.5 mol %), various substrates, including aryl- and alkyl-substituted oxindoles, were fluor
- Hamashima, Yoshitaka,Suzuki, Toshiaki,Takano, Hisashi,Shimura, Yuta,Sodeoka, Mikiko
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p. 10164 - 10165
(2007/10/03)
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- Enantioselective synthesis of BMS-204352 (MaxiPost) using N-fluoroammonium salts of cinchona alkaloids (F-CA-BF4).
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The enantioselective synthesis of a potent Maxi-K potassium channel opener (BMS-204352) mediated by N-fluoroammonium salts of cinchona alkaloids is described. Two synthetic pathways were evaluated. An ee as high as 88% was achieved (>99% after a single re
- Zoute, Ludivine,Audouard, Christophe,Plaquevent, Jean-Christophe,Cahard, Dominique
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p. 1833 - 1834
(2007/10/03)
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- Pyridazinedione compounds useful in treating neurological disorders
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The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
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- A General Method for the Synthesis of Isatins: Preparation of Regiospecifically Functionalized Isatins from Anilines
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A new method has been developed for regiospecific conversion of substituted anilines to isatins.The method utilizes the reaction of an ortho-lithiated, protected aniline derivative with diethyl oxalate to furnish an α-ketoester.Hydrolytic deprotection of the amino moiety is accompanied by cyclization to provide the isatin.
- Hewawasam, Piyasena,Meanwell, Nicholas A.
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p. 7303 - 7306
(2007/10/02)
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