1036380-75-2Relevant articles and documents
Cu-Catalyzed Denitrogenative Transannulation of 3-Aminoindazoles to Assemble 1-Aminoisoquinolines and 3-Aminobenzothiophenes
Zhou, Yao,Wang, Ya,Lou, Yixian,Song, Qiuling
, p. 8869 - 8873 (2019)
We disclose a novel Cu-catalyzed denitrogenative transannulation of 3-aminoindazoles to afford diverse functionalized 3-aminobenzothiophenes and 1-aminoisoquinolines, in which denitrogenative transannulation of 3-aminoindazoles is reported for the first t
Selective Bisubstrate Inhibitors with Sub-nanomolar Affinity for Protein Kinase Pim-1
Ekambaram, Ramesh,Enkvist, Erki,Vaasa, Angela,Kasari, Marje,Raidaru, Gerda,Knapp, Stefan,Uri, Asko
, p. 909 - 913 (2013)
Potent and selective: The unique nature of the ATP binding pocket structure of Pim family protein kinases (PKs) was used for the development of bisubstrate inhibitors and a fluorescent probe with sub-nanomolar affinity. Conjugates of arginine-rich peptides with two ATP mimetic scaffolds were synthesized and tested as inhibitors of Pim-1. Against a panel of 124 protein kinases, a novel ARC-PIM conjugate selectively inhibited PKs of the Pim family. Copyright
BENZENE FUSED HETEROCYCLIC COMPOUND AND USE THEREOF
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Paragraph 0280; 0281; 0283; 0284, (2019/06/17)
The present disclosure provides a benzene fused heterocyclic compound of Formula (I): wherein (A) is a single or double bond; n is 0 or 1; X is -CH2-, O, NR1, or S; A is -C(Ra1)(Ra2)(Ra3) or -N(R
2-Amino-4-aryl thiazole: A promising scaffold identified as a potent 5-LOX inhibitor
Sinha, Shweta,Sravanthi,Yuvaraj,Manju,Doble, Mukesh
, p. 19271 - 19279 (2016/03/01)
Human 5-lipoxygenase (5-LOX) is an important enzyme in the biosynthesis of leukotrienes and is a target for asthma and allergy treatment. Zileuton is the only drug currently marketed that targets this enzyme (IC50 ~ 1 μM). So, the development of novel lead compounds is highly desirable. A series of 2-aryl indole, thiazolopyrazole acid, oxadiazolobenzothiophene, 1,4-disubstituted-1,2,3-triazole, 2-amino-4-aryl thiazole and 4,4′-(1,4-phenylene)bis(1,3-thiazole) derivatives when tested against this enzyme resulted in the identification of a potent compound (1d), p-fluoro substituted 2-amino-4-aryl thiazole, with an IC50 of ~10 μM. Another lead compound identified is (4a), a thiazolopyrazole acid derivative (IC50 ~ 40 μM). All the compounds exhibit poor DPPH radical scavenging activity which suggests that their action occurs not due to the disruption of the redox cycle of iron present in the enzyme (unlike zileuton) but through competitive inhibition, since the Vmax remains constant but the Km increases with an increase in inhibitor concentration. Molecular docking of 1d and 4a to the active site of 5-LOX also supports the experimental data, and suggests that their possible mechanism of action is through competitive inhibition. The current study identifies a promising lead molecule which could be improved further to match the activity of the commercial drug.
Microwave-assisted synthesis of 3-aminobenzo[b]thiophene scaffolds for the preparation of kinase inhibitors
Bagley, Mark C.,Dwyer, Jessica E.,Molina, Maria D. Beltran,Rand, Alexander W.,Rand, Hayley L.,Tomkinson, Nicholas C. O.
, p. 6814 - 6824 (2015/06/25)
Microwave irradiation of 2-halobenzonitriles and methyl thioglycolate in the presence of triethylamine in DMSO at 130°C provides rapid access to 3-aminobenzo[b]thiophenes in 58-96% yield. This transformation has been applied in the synthesis of the thieno
Tricyclic aminopyrimidine histamine H4 receptor antagonists
Savall, Brad M.,Gomez, Laurent,Chavez, Frank,Curtis, Michael,Meduna, Steven P.,Kearney, Aaron,Dunford, Paul,Cowden, Jeffery,Thurmond, Robin L.,Grice, Cheryl,Edwards, James P.
scheme or table, p. 6577 - 6581 (2011/12/04)
This report discloses the development of a series of tricyclic histamine H4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H4 receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.
Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases
Tao, Zhi-Fu,Hasvold, Lisa A.,Leverson, Joel D.,Han, Edward K.,Guan, Ran,Johnson, Eric F.,Stoll, Vincent S.,Stewart, Kent D.,Stamper, Geoff,Soni, Nirupama,Bouska, Jennifer J.,Luo, Yan,Sowin, Thomas J.,Lin, Nan-Horng,Giranda, Vincent S.,Rosenberg, Saul H.,Penning, Thomas D.
experimental part, p. 6621 - 6636 (2010/05/02)
Pim-1, Pim-2, and Pim-3 are a family of serine/threonine kinases which have been found to be overexpressed in a variety of hematopoietic malignancies and solid tumors. Benzothienopyrimidinones were discovered as a novel class of Pim inhibitors that potent
PIM KINASE INHIBITORS AS CANCER CHEMOTHERAPEUTICS
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Page/Page column 8, (2008/12/06)
Inhibitors of Pim kinases, ways to make them and methods of treating patients using them are disclosed.
PIM KINASE INHIBITORS AS CANCER CHEMOTHERAPEUTICS
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Page/Page column 9, (2008/12/06)
Inhibitors of Pim kinases, ways to make them and methods of treating patients using them are disclosed.