53512-46-2Relevant articles and documents
Synthesis and biological evaluation of isomeric methoxy substitutions on anti-cancer indolyl-pyridinyl-propenones: Effects on potency and mode of activity
Trabbic, Christopher J.,George, Sage M.,Alexander, Evan M.,Du, Shengnan,Offenbacher, Jennifer M.,Crissman, Emily J.,Overmeyer, Jean H.,Maltese, William A.,Erhardt, Paul W.
, p. 79 - 91 (2016/07/06)
Certain indolyl-pyridinyl-propenone analogues kill glioblastoma cells that have become resistant to conventional therapeutic drugs. Some of these analogues induce a novel form of non-apoptotic cell death called methuosis, while others primarily cause micr
Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without Cox inhibitory activity
Arisawa, Mitsuhiro,Kasaya, Yayoi,Obata, Tohru,Sasaki, Takuma,Nakamura, Tomonori,Araki, Takuya,Yamamoto, Koujirou,Sasaki, Akito,Yamano, Akihito,Ito, Mika,Abe, Hiroshi,Ito, Yoshihiro,Shuto, Satoshi
, p. 8152 - 8163 (2012/11/07)
We designed and synthesized conformationally restricted analogues and regioisomers of the nonsteroidal anti-inflammatory drug indomethacin. Evaluation of the inhibitory effects of these compounds on COX, P-glycoprotein, and multidrug resistance indicated that NSAIDS modulation of multidrug-resistant P-glycoprotein and multidrug-resistant protein-1 is not associated with COX-1 and COX-2 inhibitory activities.
FAAH INHIBITORS
-
Page/Page column 131, (2012/07/13)
The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the com
PIPERIDINYLHYDROXYETHYLPIPERIDINES AS MODULATORS OF CHEMOKINE RECEPTORS
-
Page/Page column 21, (2009/05/28)
The present invention relates to a compound of the formula (I), or a pharmaceutically acceptable salt thereof, wherein R1-R8 and X, m, and n are defined. Compounds and compositions of the present invention are useful the treatment of atherosclerosis.
3-ACYLINDOLE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
-
Page/Page column 8-9, (2008/12/08)
The invention relates to compounds of formula (I), wherein X, R1, R2, R3, R4 and R5 are as described herein. The invention also includes preparative methods for the preparation of compounds of formula
Synthesis of 2-substituted benzofurans and indoles using functionalized titanium benzylidene reagents on solid phase
Macleod, Calum,McKiernan, Gordon J.,Guthrie, Emma J.,Farrugia, Louis J.,Hamprecht, Dieter W.,Macritchie, Jackie,Hartley, Richard C.
, p. 387 - 401 (2007/10/03)
Titanium(IV) benzylidenes bearing a masked oxygen or nitrogen nucleophile in the ortho position were generated from thioacetals, using low-valent titanocene complex, Cp2Ti[P(OEt)3]2. Methylene acetal, alkyl ether, silyl ether, fluoro, tertiary amino, and N-alkyl, N-benzyl, N-prenyl, and N-silyl tert-butyl carbamate groups were tolerated in the titanium alkylidene reagents (Schrock carbenes). Aryl-chlorine bonds were stable to the titanium benzylidene functionality, but there was poor chemoselectivity for the reduction of the thioacetal in the presence of an aryl chloride. The titanium benzylidenes converted Merrifield and Wang resin-bound esters into enol ethers. The oxygen nucleophile was masked as a TMS ether, and when the resin-bound enol ethers bearing this ortho substituent were treated with 1% TFA in dichloromethane, benzofurans were released from resin in high yields. The chameleon catch strategy ensured excellent purity. In a similar way, N-alkylated and N-silylated tert-butyl carbamates were used for the synthesis of N-alkyl and N-Boc indoles, respectively. These traceless solid-phase syntheses of heterocycles are believed to involve post-cleavage modification rather than cyclative termination.
Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
-
, (2008/06/13)
Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leukocyte-activation associated diseases comprise compounds of formula (I), in which A and B are nitrogen or carbon, provided only one of A and B is nitrogen; and R1-R6 are as defined in the specification, wherein R2 with R5 may form a ring, and/or two R4 groups may form a six-membered aryl or heteroaryl ring, optionally having a substituent R6 forming a ring with R3.
A general large scale synthesis of 2-alkyl-7-methoxyindoles
Chen, Bang-Chi,Hynes Jr., John,Pandit, Chennagiri R.,Zhao, Rulin,Skoumbourdis, Amanda P.,Wu, Hong,Sundeen, Joseph E.,Leftheris, Katerina
, p. 951 - 960 (2007/10/03)
A general method has been developed for the large scale synthesis of 2-alkyl-7-methoxyindoles and analogs. This method involves an efficient preparation of the key intermediates, 1-(2-nitroaryl)-2-nitroalkanols and 1-(2-nitroaryl)-2-nitroalkenes, and affords 2-alkyl-7-methoxyindoles and analogs in 3 steps with good overall yields.