31009-04-8Relevant academic research and scientific papers
Quinoline formamide compound as well as preparation method and application thereof
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Paragraph 0130-0132; 0136-0138; 0175-0177; 0181-0183, (2020/11/25)
The invention discloses quinoline formamide compounds as well as a preparation method and application thereof. Specifically, the invention relates to a compound represented by a formula (I) as shown in the specification or a tautomer, a meso-racemate, a r
Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma
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
, p. 516 - 530 (2018/06/15)
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.
NOVEL FAP INHIBITORS
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Paragraph 0365; 0432, (2014/12/09)
The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
Selective inhibitors of fibroblast activation protein (FAP) with a (4-quinolinoyl)-glycyl-2-cyanopyrrolidine scaffold
Jansen, Koen,Heirbaut, Leen,Cheng, Jonathan D.,Joossens, Jurgen,Ryabtsova, Oxana,Cos, Paul,Maes, Louis,Lambeir, Anne-Marie,De Meester, Ingrid,Augustyns, Koen,Van Der Veken, Pieter
, p. 491 - 496 (2013/07/19)
Fibroblast activation protein (FAP) is a serine protease that is generally accepted to play an important role in tumor growth and other diseases involving tissue remodeling. Currently there are no FAP inhibitors with reported selectivity toward both the closely related dipeptidyl peptidases (DPPs) and prolyl oligopeptidase (PREP). We present the discovery of a new class of FAP inhibitors with a N-(4-quinolinoyl)-Gly-(2-cyanopyrrolidine) scaffold. We have explored the effects of substituting the quinoline ring and varying the position of its sp2 hybridized nitrogen atom. The most promising inhibitors combined low nanomolar FAP inhibition and high selectivity indices (>10 3) with respect to both the DPPs and PREP. Preliminary experiments on a representative inhibitor demonstrate that plasma stability, kinetic solubility, and log D of this class of compounds can be expected to be satisfactory.
NOVEL FAP INHIBITORS
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Page/Page column 57, (2013/07/31)
The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
Facile and efficient synthesis of quinoline-4-carboxylic acids under microwave irradiation
Zhu, Hui,Yang, Ri Fang,Yun, Liu Hong,Li, Jin
experimental part, p. 35 - 38 (2010/11/04)
A facile and efficient method for the preparation of 2-non-substituted quinoline-4-carboxylic acids is described via the Pfitzinger reaction of isatins with sodium pyruvate following consequent decarboxylation under microwave irradiation.
