954232-88-3Relevant academic research and scientific papers
Effective synthesis of benzimidazoles-imidazo[1,2-a]pyrazine conjugates: A comparative study of mono-and bis-benzimidazoles for antitumor activity
Singh, Iqubal,Luxami, Vijay,Paul, Kamaldeep
, p. 546 - 561 (2019/08/01)
A novel series of 6-substituted-8-(1-cyclohexyl-1H-benzo[d]imidazole-6-yl)imidazo[1,2-a]pyrazine and 6-substituted-8-(1-benzyl-1H-benzo[d]imidazole-6-yl)imidazo[1,2-a]pyrazine is first time synthesized and screen in vitro biological activity for 60 human cancer cell lines representing nine different cancer types. Derivatives 10 and 36 show antitumor activity for all tested cell lines, display comparable full panel mean-graph midpoint growth inhibition (MG_MID GI50) values of 2.10 and 2.23 μM, respectively. Furthermore, these derivatives show strong binding interactions with DNA and bovine serum albumin (BSA), studied through absorption, emission, and circular dichroism techniques. These spectroscopic studies reveal that imidazo[1,2-a]pyrazine-benzimidazoles 10 and 36, intercalate with ct-DNA as a leading interaction for fundamental biologically significant effects, with monobenzimidazole show better activity than bisbenzimidazole. These experiments have confirmed that the imidazo[1,2-a]pyrazine and benzimidazole moieties are efficient pharmacophores to trigger binding to DNA. These compounds have also interacted with bovine serum albumin protein that demonstrating high values of binding constant.
NOVEL BICYCLIC BROMODOMAIN INHIBITORS
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Paragraph 0203, (2015/01/16)
The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 00353, (2014/07/08)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described
ANTI-AMYLOID COMPOUNDS AND METHODS
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Page/Page column 39, (2012/09/21)
Anti-amyloid compounds are provided along with methods of use thereof.
The development of benzimidazoles as selective rho kinase inhibitors
Sessions, E. Hampton,Smolinski, Michael,Wang, Bo,Frackowiak, Bozena,Chowdhury, Sarwat,Yin, Yan,Chen, Yen Ting,Ruiz, Claudia,Lin, Li,Pocas, Jennifer,Schr?ter, Thomas,Cameron, Michael D.,LoGrasso, Philip,Feng, Yangbo,Bannister, Thomas D.
scheme or table, p. 1939 - 1943 (2010/09/03)
Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC50 10 nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
