896722-53-5Relevant academic research and scientific papers
Cu(II)-catalyzed sulfonylation of 7-azaindoles using DABSO as SO2-Source and its mechanistic study
Urvashi,Dar, Mohammad Ovais,Bharatam, Prasad V.,Das, Parthasarathi,Kukreti, Shrikant,Tandon, Vibha
, (2020/06/23)
DABSO mediated sulfonylation of iodinated 7-azaindoles was achieved for the first time through sulfonylative Suzuki-Miyaura cross coupling (SMC) reaction under mild conditions giving good yields of sulfonylated 7-azaindole derivatives. Interestingly, control experiments suggest that present method involves in-situ generation of ArSO2 free radical followed by the key steps of SMC reaction. Scope of the reaction was explored with both electronically different and bulky group carrying boronic acids as coupling partner. The sulfonylation is scalable and occurred selectively at iodo group, irrespective of its position on azaindole. Moreover, the proposed mechanism has been supported by electron paramagnetic resonance (EPR) and density functional theory (DFT) calculations.
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: Lead optimization
Alonso, Juan Antonio,Andrs, Miriam,Bravo, Mnica,Calbet, Marta,Eastwood, Paul R.,Eichhorn, Peter,Esteve, Cristina,Ferrer, Manel,Gmez, Elena,Gonzlez, Jacob,Mir, Marta,Moreno, Imma,Petit, Silvia,Roberts, Richard S.,Sevilla, Sara,Vidal, Bernat,Vidal, Laura,Vilaseca, Pere,Zanuy, Miriam
, p. 5123 - 5126 (2015/01/08)
Extensive structure-activity relationship (SAR) and structure-kinetic relationship (SKR) studies in the bicyclic heteroaromatic series of CRTh2 antagonists led to the identification of several molecules that possessed both excellent binding and cellular potencies along with long receptor residence times. A small substituent in the bicyclic core provided an order of magnitude jump in dissociation half-lives. Selected optimized compounds demonstrated suitable pharmacokinetic profiles.
Scaffold-hopping strategy: Synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents
Tung, Yen-Shih,Coumar, Mohane Selvaraj,Wu, Yu-Shan,Shiao, Hui-Yi,Chang, Jang-Yang,Liou, Jing-Ping,Shukla, Paritosh,Chang, Chun-Wei,Chang, Chi-Yen,Kuo, Ching-Chuan,Yeh, Teng-Kuang,Lin, Chin-Yu,Wu, Jian-Sung,Wu, Su-Ying,Liao, Chun-Chen,Hsieh, Hsing-Pang
supporting information; experimental part, p. 3076 - 3080 (2011/06/25)
Utilizing scaffold-hopping drug-design strategy, we sought to identify a backup drug candidate for BPR0L075 (1), an indole-based anticancer agent. For this purpose, 5,6-fused bicyclic heteroaromatic scaffolds were designed and synthesized through shufflin
Design and synthesis of 1-(2-alkanamidoethyl)-6-methoxy-7-azaindole derivatives as potent melatonin agonists
Jeanty, Matthieu,Suzenet, Franck,Delagrange, Philippe,Nosjean, Olivier,Boutin, Jean A.,Caignard, Daniel H.,Guillaumet, Gérald
supporting information; experimental part, p. 2316 - 2319 (2011/05/15)
A series of 7-azaindolic ligands bearing a methoxy group and a N-acetyl chain as melatoninergic pharmacophores were synthesized and their binding affinities towards MT1 and MT2 receptors were evaluated. Compounds 7a-c and 12 (cyclohe
The first practical and efficient one-pot synthesis of 6-substituted 7-azaindoles via a Reissert-Henze reaction
Storz, Thomas,Bartberger, Michael D.,Sukits, Steven,Wilde, Chris,Soukup, Troy
, p. 201 - 214 (2008/12/21)
A variety of 6-substituted 7-azaindoles (30 examples) were obtained via selective O-methylation of 7-azaindole-N-oxide m-chlorobenzoic acid salt and subsequent, base-catalyzed one-pot reaction with a range of N-, O-, S-nucleophiles or cyanide. Georg Thieme Verlag Stuttgart.
COMPOUNDS AND METHODS OF USE
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Page/Page column 135-136, (2010/11/27)
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Anti-tumor compounds
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Page/Page column 11, (2008/06/13)
Compounds of the following formula: wherein A, D, Q, T, U, V, W, X, Y, Z, R1, and ---- are as defined herein. This invention also relates to a method of inhibiting tubulin polymerization, or treating cancer or an angiogenesis-related disorder w
