Synthesis and structure–activity relationships of N2-alkylated quaternary β-carbolines as novel antitumor agents
摘要:
A series of novel N-2-alkylated quaternary beta-carbolines was synthesized by modification of position-1, 2,7 and 9 of beta-carboline nucleus with various alkyl and arylated alkyl substituents, and their cytotoxic activities in vitro and antitumor potencies in mice were evaluated. Compound 3m was found to be the most potent antitumor agent. SARs analysis revealed that (1) the substituents in position-2 and 9 of beta-carboline nucleus played a vital role in modulation of antitumor activity; (2) the benzyl and 3-phenylpropyl substituents in position-2 and 9 of beta-carboline ring were the optimal substituents giving rise to significant antitumor agent. These compounds might be a novel promising class of antitumor agents with clinical development potential. (C) 2013 Elsevier Masson SAS. All rights reserved.
Synthesis and structure–activity relationships of N2-alkylated quaternary β-carbolines as novel antitumor agents
摘要:
A series of novel N-2-alkylated quaternary beta-carbolines was synthesized by modification of position-1, 2,7 and 9 of beta-carboline nucleus with various alkyl and arylated alkyl substituents, and their cytotoxic activities in vitro and antitumor potencies in mice were evaluated. Compound 3m was found to be the most potent antitumor agent. SARs analysis revealed that (1) the substituents in position-2 and 9 of beta-carboline nucleus played a vital role in modulation of antitumor activity; (2) the benzyl and 3-phenylpropyl substituents in position-2 and 9 of beta-carboline ring were the optimal substituents giving rise to significant antitumor agent. These compounds might be a novel promising class of antitumor agents with clinical development potential. (C) 2013 Elsevier Masson SAS. All rights reserved.
BETA-CARBOLINES FOR USE IN THE TREATMENT OF HEARING LOSS AND VERTIGO
申请人:Rommelspacher Hans
公开号:US20130028958A1
公开(公告)日:2013-01-31
The present invention is directed at β-carbolines, preferred 9-alkyl-β-carbolines (
9
-alkyl-β-BC), their manufacture as well as their use in prophylaxis and treatment of hearing damages, tinnitus, acute acoustic trauma, vertigo and vestibular disorder as well as pharmaceutical compositions containing theses β-carbolines.
The present invention relates to fluoro-9-methyl-β-carbolines, their preparation as well as their medical use and pharmaceutical compositions containing fluoro-9-methyl-β-carbolines.
B-CARBOLINE FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
申请人:Rommelspacher Hans
公开号:US20100143474A1
公开(公告)日:2010-06-10
The embodiments relate to derivatives of 9-alkyl-β-carboline, their production and pharmaceutical compositions containing these 9-alkyl-β-carboline derivatives. Further, the use of 9-alkyl-β-carboline derivatives and pharmaceutical compositions for the treatment and prevention of movement disorders, neurodegenerative diseases, Alzheimer's disease and Parkinson's disease is described. Additionally, these effects can be utilized for the cultivation of cells such as dopaminergic cells or stem cells which shall be engrafted for the treatment of Parkinson's disease.
STABLE POLYMORPHIC FORM OF 6-FLUORO-9-METHYL-9H-SS-CARBOLINE AND USES THEREOF
申请人:Audiocure Pharma GmbH
公开号:EP3772515A1
公开(公告)日:2021-02-10
The present invention relates to a stable crystalline polymorphic form of 6-fluoro-9-methyl-9H-β-carboline of formula (I)
a method for preparation of said crystalline polymorphic form of 6-fluoro-9-methyl-9H-β-carboline, and a pharmaceutical composition comprising said crystalline polymorphic form of 6-fluoro-9-methyl-9H-β-carboline. Furthermore, the present invention relates to the use of said stable crystalline polymorphic form and the use of the pharmaceutical composition comprising said stable crystalline polymorphic form in the treatment and/or prophylaxis of hearing damage, vertigo or vestibular disorders.