613679-11-1Relevant academic research and scientific papers
A general and scalable synthesis of polysubstituted indoles
Diana-Rivero, Raquel,García-Tellado, Fernando,Tejedor, David
, (2021/06/14)
A consecutive 2-step synthesis of N-unprotected polysubstituted indoles bearing an electron-withdrawing group at the C-3 position from readily available nitroarenes is reported. The protocol is based on the [3,3]-sigmatropic rearrangement of N-oxyenamines generated by the DABCO-catalyzed reaction of N-arylhydroxylamines and conjugated terminal alkynes, and delivers indoles endowed with a wide array of substitution patterns and topologies.
Decarboxylative acylation of: N -free indoles enabled by a catalytic amount of copper catalyst and liquid-assisted grinding
Yu, Jingbo,Zhang, Chao,Yang, Xinjie,Su, Weike
supporting information, p. 4446 - 4451 (2019/05/16)
A facile decarboxylative acylation of N-free indoles with α-ketonates via liquid-assisted grinding was reported. The reaction requires only a catalytic amount of Cu(OAc)2·H2O in combination with O2 as the terminal oxidant to give various 3-acylindoles with high efficiency. Additionally, this new methodology was applicable to a gram-scale synthesis.
Synthesis of 3-acylindoles by oxidative rearrangement of 2-aminochalcones using a hypervalent iodine reagent and cyclization sequence
Nakamura, Akira,Tanaka, Satoshi,Imamiya, Akira,Takane, Reo,Ohta, Chiaki,Fujimura, Kazuma,Maegawa, Tomohiro,Miki, Yasuyoshi
supporting information, p. 6702 - 6705 (2017/08/22)
An efficient one-pot method was developed for the construction of 3-acylindoles via oxidative rearrangement of 2-aminochalcones followed by intramolecular cyclization. The reaction was used to convert a variety of 2-aminochalcones into 3-acylindoles in mo
Palladium catalyzed addition of arylboronic acid or indole to nitriles: Synthesis of aryl ketones
Das, Tuluma,Chakraborty, Amarnath,Sarkar, Amitabha
supporting information, p. 7198 - 7202 (2015/01/09)
Aryl ketones can be synthesized conveniently by a palladium catalyzed addition of arylboronic acid to nitriles in aqueous triflic acid. This catalytic system was extended to the addition of unprotected indoles to nitriles under a slightly modified condition to produce 3-acyl indoles in good yields.
S1P RECEPTORS MODULATORS
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Page/Page column 63, (2010/04/30)
The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
Synthesis and biological evaluation of (3,4,5-trimethoxyphenyl)indol-3-ylmethane derivatives as potential antivascular agents
Dupeyre, Gregory,Chabot, Guy G.,Thoret, Sylviane,Cachet, Xavier,Seguin, Johanne,Guenard, Daniel,Tillequin, Francois,Scherman, Daniel,Koch, Michel,Michel, Sylvie
, p. 4410 - 4426 (2007/10/03)
Combretastatin A-4 (CSA-4), a stilbene derivative, is a potent vascular disrupting agent (VDA) with the structural requirement of a cis-configuration to maintain a molecular geometry and a correct orientation of both phenyl groups. A series of indolic ana
Indole compounds
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, (2008/06/13)
This invention relates to methods of inhibiting tubulin polymerization and treating cancer and other angiogenesis-related disorders with indole compounds of the formula: wherein L1, L2, R1, R2, Ra, R
Indole compounds
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, (2008/06/13)
Indole compounds of the formula: wherein L1, L2, R1, R2, Ra, Rb, Rc, Rd, and Re are defined herein. Also disclosed are methods of using of the indole compou
Indole compounds as inhibitors of tubulin polymerisation for the treatment of angiogenesis-related disorders
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Page/Page column 11, (2010/02/10)
Indole compounds of the formula: wherein L1 is CO; L2 is a bond; R1 is aryl or heteroaryl; R2 is H, aryl, heteroaryl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRR', SO2
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents
Liou, Jing-Ping,Chang, Yi-Ling,Kuo, Fu-Ming,Chang, Chun-Wei,Tseng, Huan-Yi,Wang, Chiung-Chiu,Yang, Yung-Ning,Chang, Jang-Yang,Lee, Shiow-Ju,Hsieh, Hsing-Pang
, p. 4247 - 4257 (2007/10/03)
The synthesis and study of the structure-activity relationships of two new classes of synthetic antitubulin compounds based on 1-aroylindole and 3-aroylindole skeletons are described. Lead compounds 3, 10, and 14 displayed potent cytotoxicities with ICsu
