1186293-68-4Relevant academic research and scientific papers
Compounds with coumarin-biphenyl skeleton, and preparation method and application of compounds
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Paragraph 0038; 0070-0071, (2019/09/14)
The invention belongs to the field of pharmaceutical chemistry, and discloses compounds with a coumarin-biphenyl skeleton, and a preparation method and application of the compounds. The compounds havefollowing structural general formulae. The preparation method of the two compounds is simple and reliable, and the total yield is 40% or above. Preliminary pharmacological experiments show that the compounds have a certain relaxation effect on an in-vitro arterial blood vessel of a rat, and can be used for development of antihypertensive drugs.
Synthesis and biological evaluation of coumarin-1,2,3-triazole- dithiocarbamate hybrids as potent LSD1 inhibitors
Ye, Xian-Wei,Zheng, Yi-Chao,Duan, Ying-Chao,Wang, Meng-Meng,Yu, Bin,Ren, Jing-Li,Ma, Jin-Lian,Zhang, En,Liu, Hong-Min
supporting information, p. 650 - 654 (2014/05/06)
Two series of coumarin-1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for their inhibitory activity towards lysine specific demethylase 1 (LSD1). Compounds 8a, 8d-8f, 8i-8l presented potent activity against lysine specific demethylase 1. Among them, compound 8k showed potent and reversible inhibition against lysine specific demethylase 1 with an IC50 value of 0.39 μM, which was 74-fold more potent than that of tranylcypromine (2-PCPA). Besides, compound 8k displayed excellent selectivity against lysine specific demethylase 1 without inhibition against monoamine oxidases (MAOs) A and B. Further investigation revealed that compound 8k was active at both recombinant and cell levels by upregulating the expression of H3K4me1, H3K4me2 and H3K9me2. This journal is the Partner Organisations 2014.
A macrocyclic coumarin-containing tripeptide via CuAAC chemistry
Van Berkel, Sander S.,Van Der Lee, Bas,Van Delft, Floris L.,Rutjes, Floris P. J. T.
supporting information; experimental part, p. 4272 - 4274 (2011/03/19)
A Cu-catalysed macrocyclisation was performed to obtain a macrocyclic coumarin-containing tripeptide for use in thrombin activity measurements.
