866848-94-4Relevant academic research and scientific papers
HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
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Paragraph 0647-0648, (2021/02/25)
The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
INHIBITORS OF HIV-1 ENTRY AND METHODS OF USE THEREOF
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Page/Page column 49, (2016/02/29)
The disclosure provides compositions and methods for sensitizing primary HIV-1, including transmitted/founder viruses, to neutralization by monoclonal antibodies, e.g., those directed against CD4-induced (CD4i) epitopes and the V3 region. In certain embodiments, the disclosure relates to the use of small molecules as microbicides to inhibit HIV-1 infection directly and to sensitize primary HIV-1 to neutralization by readily elicited antibodies.
Small-Molecule CD4-Mimics: Structure-Based Optimization of HIV-1 Entry Inhibition
Melillo, Bruno,Liang, Shuaiyi,Park, Jongwoo,Sch?n, Arne,Courter, Joel R.,Lalonde, Judith M.,Wendler, Daniel J.,Princiotto, Amy M.,Seaman, Michael S.,Freire, Ernesto,Sodroski, Joseph,Madani, Navid,Hendrickson, Wayne A.,Smith, Amos B.
supporting information, p. 330 - 334 (2016/03/22)
The optimization, based on computational, thermodynamic, and crystallographic data, of a series of small-molecule ligands of the Phe43 cavity of the envelope glycoprotein gp120 of human immunodeficiency virus (HIV) has been achieved. Importantly, biological evaluation revealed that the small-molecule CD4 mimics (4-7) inhibit HIV-1 entry into target cells with both significantly higher potency and neutralization breadth than previous congeners, while maintaining high selectivity for the target virus. Their binding mode was characterized via thermodynamic and crystallographic studies.
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors
Dinges, Juergen,Akritopoulou-Zanze, Irini,Arnold, Lee D.,Barlozzari, Teresa,Bousquet, Peter F.,Cunha, George A.,Ericsson, Anna M.,Iwasaki, Nobuhiko,Michaelides, Michael R.,Ogawa, Nobuo,Phelan, Kathleen M.,Rafferty, Paul,Sowin, Thomas J.,Stewart, Kent D.,Tokuyama, Ryukou,Xia, Zhiren,Zhang, Henry Q.
, p. 4371 - 4375 (2007/10/03)
A series of 1,4-dihydroindeno[1,2-c]pyrazoles was prepared and evaluated for their enzymatic inhibition of KDR kinase. Computer modeling studies revealed the importance of attaching a basic side chain in predicting the binding mode of those compounds. Fur
TRICYCLIC PYRAZOLE KINASE INHIBITORS
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Page/Page column 59, (2008/06/13)
Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
