866848-94-4Relevant articles and documents
HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
-
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.
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.
TRICYCLIC PYRAZOLE KINASE INHIBITORS
-
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.