223690-87-7Relevant academic research and scientific papers
beta-carboline derivative, preparation method thereof and application of beta-carboline derivate in preparation of antitumor drugs
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Paragraph 0021, (2019/04/17)
The invention discloses a methyl 6-chloro-9-methyl-9H-beta-carboline-3-carboxylate derivative with a structure of general formula (I), which is shown in the description, or its pharmaceutically acceptable salt, a preparation method thereof, and application of the derivative or its pharmaceutically acceptable salt in the preparation of antitumor drugs, wherein R1, R2 and R3 are defined the same asin the description.
A practical synthesis of β-carbolines by tetra-n-butylammonium bromide (TBAB)-mediated cycloaromatization reaction of aldehydes with tryptophan derivatives
Wang, Zhen,Yu, Zhenzhen,Yao, Yao,Zhang, Yakai,Xiao, Xuefeng,Wang, Bin
supporting information, p. 1541 - 1544 (2019/07/22)
A mild and efficient nBu4NBr-mediated oxidative cycloaromatization to prepare β-carbolines from readily available tryptophans and aldehydes is described. The reaction is practical and allows the synthesis of β-carbolines on gram-scale. Some of
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy
Srivastava, Sanjay K.,Agarwal, Alka,Chauhan, Prem M. S.,Agarwal, Shiv K.,Bhaduri, Amiya P.,Singh, Som N.,Fatima, Nigar,Chatterjee, Ranjit K.
, p. 1667 - 1672 (2007/10/03)
Substituted 9H-pyrido[3,4-b]indoles (β-carbolines), identified in our laboratory as potential pharmacophores for designing macrofilaricidal agents, have been explored further for identifying the pharmacophore responsible for the high order of adulticidal
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy
Srivastava,Agarwal,Chauhan,Agarwal,Bhaduri,Singh,Fatima,Chatterjee
, p. 1223 - 1236 (2007/10/03)
Substituted 9H-pyrido[3,4-b]indoles (β-carbolines) identified in our laboratory as potential pharmacophore for designing macrofilaricidal agents, have been explored further for identifying the pharmacophore responsible for high order of adulticidal activity. This has led to syntheses and macrofilaricidal evaluations of a number of 1-aryl-9H-pyrido[3,4-b]indole-3-carboxylate derivatives (3-7). The macrofilarical activity was initially evaluated in vivo against Acanthoeilonema viteae. Amongst all the synthesized compounds, only twelve compounds namely 3a, 3c, 3d, 3f, 4c, 4d, 4f, 5a, 6f, 6h, 6i and 7h have exhibited either >90% micro- or macrofilaricidal activity or sterilization of female worms. These compounds have also been screened against Litomosoides carinii and of these only 3f and 5a have also been found to be active. Finally these two compounds have been evaluated against Brugia malayi. The structure activity relationship (SAR) associated with position-1 and 3 substituents in β-carbolines have been discussed. It has been observed that the presence of carbomethoxy at position-3 and an aryl substituent at position-1 in β-carbolines effectively enhance antifilarial activity particularly against A. viteae. Amongst the various compounds screened, methyl 1-(4-methylphenyl)-9H-pyrido[3,4-b]indole-3-carboxylate (4c) has shown highest adulticidal activity and methyl 1-(4-chlorophenyl)-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indole-3-carboxylate (3a) has shown highest microfilaricidal action against A. viteae at 50mg/kgx5 days (ip). Another derivative of this compound namely 1-(4-chlorophenyl)-3-hydroxymethyl-9H-pyrido[3,4-b]indole (5a) exhibited highest activity against L. carinii at 30mg/kgx5 days (ip) and against B. malayi at 50mg/kgx5 days (ip) or at 200mg/kgx5 days (po). Copyright (C) 1999 Elsevier Science Ltd.
