915411-18-6Relevant academic research and scientific papers
CARBOLINE DERIVATIVE SERVING AS BROMODOMAIN INHIBITOR
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Paragraph 0188; 0189, (2018/12/07)
Disclosed in the present invention is a carboline derivative serving as an bromodomain inhibitor. The carboline derivative in the present invention can be used as an bromodomain inhibitor, and can provide a method and a pharmaceutical composition for controlling diseases intervened by a bromodomain protein.
PROBES FOR IMAGING HUNTINGTIN PROTEIN
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Paragraph 0218, (2016/03/22)
Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.
Synthesis and pharmacological evaluation of N -(3-(1 H -Indol-4-yl)-5-(2- methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent
Shetty, Rupa S.,Lee, Younghee,Liu, Bin,Husain, Arifa,Joseph, Rhoda W.,Lu, Yixin,Nelson, David,Mihelcic, John,Chao, Wenchun,Moffett, Kristofer K.,Schumacher, Andreas,Flubacher, Dietmar,Stojanovic, Aleksandar,Bukhtiyarova, Marina,Williams, Ken,Lee, Kyoung-Jin,Ochman, Alexander R.,Saporito, Michael S.,Moore, William R.,Flynn, Gary A.,Dorsey, Bruce D.,Springman, Eric B.,Fujimoto, Ted,Kelly, Martha J.
experimental part, p. 179 - 200 (2011/03/19)
The synthesis and optimization of a series of orally bioavailable 1-(1H-indol-4-yl)-3,5-disubstituted benzene analogues as antimitotic agents are described. A functionalized dibromobenzene intermediate was used as a key scaffold, which when modified by sequential Suzuki coupling and Buchwald-Hartwig amination provided a flexible entry to 1,3,5-trisubstituted phenyl compounds. A 1H-indol-4-yl moiety at the 1-position was determined to be a critical feature for optimal potency. The compounds have been shown to induce cell cycle arrest at the G2/M phase and demonstrate efficacy in both cell viability and cell proliferation assays. The primary site of action for these agents is revealed by their colchicine competitive inhibition of tubulin polymerization, and a computational model has been developed for the association of these compounds to tubulin. An optimized lead LP-261 significantly inhibits growth of a human non-small-cell lung tumor (NCI-H522) in a mouse xenograft model.
Protected indazole boronic acid pinacolyl esters: Facile syntheses and studies of reactivities in Suzuki-Miyaura cross-coupling and hydroxydeboronation reactions
Crestey, Fran?ois,Lohou, Elodie,Stiebing, Silvia,Collot, Valérie,Rault, Sylvain
body text, p. 615 - 619 (2009/07/09)
The paper describes a rapid and efficient synthesis for the isolation of protected indazolylboronic esters. These compounds were synthesized by reaction between prepared protected haloindazoles and bis(pinacolato)diboron. The effects of solvent, temperature, reaction time, and the nature of halogen atom as well as protecting group were investigated. Additionaly, these compounds reacted either with aryl halides in a Suzuki-Miyaura cross-coupling reaction or with hydrogen peroxide in a hydroxydeboronation reaction showing the potential access to new aryl and hydroxyindazole libraries. Georg Thieme Verlag Stuttgart.
Anti-cancer agents and uses thereof
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Page/Page column 28-29, (2008/12/08)
The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
ANTI-CANCER AGENTS ANS USES THEREOF
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Page/Page column 75, (2010/11/29)
The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula (I): and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3 R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6- 10 carbons in the ring portion, an optionally-substituted 6- membered heteroaryl group having 1- 3 nitrogen atoms in the ring portion, an optionally-substituted 5- membered heteroaryl group having 0- 4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6- membered ring is fused either to a 5- membered ring or to a 6- membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
