20583-31-7Relevant academic research and scientific papers
Design, synthesis, in silico, and in vitro evaluation of 3-phenylpyrazole acetamide derivatives as antimycobacterial agents
Gaikwad, Nikhil B.,Nirmale, Krishna,Sahoo, Santosh K.,Ahmad, Mohammad N.,Kaul, Grace,Shukla, Manjulika,Nanduri, Srinivas,Das Gupta, Arunava,Chopra, Sidharth,Yaddanapudi, Madhavi V.
, (2020/12/23)
Mycobacterium tuberculosis (Mtb) is one of the most dangerous pathogens affecting immunocompetent and immunocompromised patients worldwide. Novel molecules, which are efficient and can reduce the duration of therapy against drug-resistant strains, are an
EXO-AZA SPIRO INHIBITORS OF MENIN-MLL INTERACTION
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Page/Page column 215, (2019/07/13)
Provided are compounds of Formula (I), pharmaceutical compositions comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes.
NOVEL FUSED PYRIDINE DERIVATIVES USEFUL AS FAK/AURORA KINASE INHIBITORS
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Page/Page column 44, (2018/02/28)
This invention relates to certain novel pyrimidine derivatives of the Formula (I). The invention also relates to process for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer.
Phenylalaninamide pesticides and a preparing method thereof
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, (2018/04/02)
The invention relates to the technical fields of organic synthesis and application techniques, and particularly relates to phenylalaninamide pesticides and a preparing method thereof. Phenylalanine, substituted phenylacetic acid, and the like are adopted
Novel crown ether functionalized imidazolium-based acidic ionic liquid catalyzed synthesis of pyrazole derivatives under solvent-free conditions
Patil, Dayanand,Chandam, Dattatraya,Mulik, Abhijeet,Jagdale, Suryabala,Patil, Prasad,Deshmukh, Madhukar
, p. 6843 - 6858 (2015/08/18)
Abstract An innovatively designed novel crown ether functionalized imidazolium-based reusable acidic ionic liquid [crown ether MIm] [HSO4] has been efficiently implemented for the synthesis of pyrazole derivatives using various substituted enaminones, hydrazine hydrate and phenyl hydrazine under solvent-free conditions. Structural novelty and task efficiency of the catalyst, high yields of desired products, greener approach attributing high atom economy and solvent-free conditions render this protocol suitable to cope with the current demand in contemporary organic chemistry. The inventive idea of utilizing crown ether functionalized ionic liquid as a catalyst was for the first time demonstrated in this protocol.
An efficient solvent-free synthesis of NH-pyrazoles from β-dimethylaminovinylketones and hydrazine on grinding
Longhi, Kelvis,Moreira, Dayse N.,Marzari, Mara R.B.,Floss, Vagner M.,Bonacorso, Helio G.,Zanatta, Nilo,Martins, Marcos A.P.
supporting information; experimental part, p. 3193 - 3196 (2010/08/05)
A series of NH-pyrazoles was efficiently synthesized from the reaction of β-dimethylaminovinylketones ([R1C(O)C(R2){double bond, long}CHN(Me2)], where R1 = Me, Ph, 3-MeO-Ph, 4-Me-Ph, 4-MeO-Ph, 4-F-Ph, 4-Cl-Ph, 4
Discovery of GSK1070916, a potent and selective inhibitor of aurora B/C kinase
Adams, Nicholas D.,Adams, Jerry L.,Burgess, Joelle L.,Chaudhari, Amita M.,Copeland, Robert A.,Donatelli, Carla A.,Drewry, David H.,Fisher, Kelly E.,Hamajima, Toshihiro,Hardwicke, Mary Ann,Huffman, William F.,Koretke-Brown, Kristin K.,Lai, Zhihong V.,McDonald, Octerloney B.,Nakamura, Hiroko,Newlander, Ken A.,Oleykowski, Catherine A.,Parrish, Cynthia A.,Patrick, Denis R.,Plant, Ramona,Sarpong, Martha A.,Sasaki, Kosuke,Schmidt, Stanley J.,Silva, Domingos J.,Sutton, David,Tang, Jun,Thompson, Christine S.,Tummino, Peter J.,Wang, Jamin C.,Xiang, Hong,Yang, Jingsong,Dhanak, Dashyant
experimental part, p. 3973 - 4001 (2010/08/07)
The Aurora kinases play critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors. Selective inhibitors may provide a new therapy for the treatment of tumors with Aurora kinase amplification. Herein we describe our lead optimization efforts within a 7-azaindole-based series culminating in the identification of GSK1070916 (17k). Key to the advancement of the series was the introduction of a 2-aryl group containing a basic amine onto the azaindole leading to significantly improved cellular activity. Compound 17k is a potent and selective ATP-competitive inhibitor of Aurora B and C with Ki* values of 0.38 ± 0.29 and 1.5 ± 0.4 nM, respectively, and is >250-fold selective over Aurora A. Biochemical characterization revealed that compound 17k has an extremely slow dissociation half-life from Aurora B (>480 min), distinguishing it from clinical compounds 1 and 2. In vitro treatment of A549 human lung cancer cells with compound 17k results in a potent antiproliferative effect (EC50 = 7 nM). Intraperitoneal administration of 17k in mice bearing human tumor xenografts leads to inhibition of histone H3 phosphorylation at serine 10 in human colon cancer (Colo205) and tumor regression in human leukemia (HL-60). Compound 17k is being progressed to human clinical trials.
Two convenient regioselective syntheses of 1-N-alkyl-3-aryl-4-[pyrimidin-4-yl]-pyrazoles
Ralph, Jeffrey M.,Faitg, Thomas H.,Silva, Domingos J.,Feng, Yanhong,Blackledge, Charles W.,Adams, Jerry L.
scheme or table, p. 1377 - 1380 (2009/06/08)
Two regioselective synthetic routes for 1-N-alkyl-3-aryl-4-[pyrimidin-4-yl]-pyrazoles of generic formula 1 were developed. These highly efficient and scalable routes circumvent the generally observed poor regioselectivity for the pyrazole alkylation.
PYRIMIDINYL-PYRAZOLE INHIBITORS OF AURORA KINASES
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Page/Page column 58-59, (2010/11/26)
The present invention provides a compound represented by Formula (I): or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a combination thereof, wherein the substituents are as defined herein. The present invention also relates to a co
AZAINDOLE INHIBITORS OF AURORA KINASES
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Page/Page column 84, (2008/06/13)
The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including s
