19837-79-7Relevant articles and documents
QUINOLINE DERIVATIVES AND USES IN MANAGING CANCER
-
, (2021/03/19)
Provided herein are compounds, pharmaceutical compositions including such compounds, and methods of using such compounds to treat diseases or disorders associated with MDM2 activity.
Experimental and theoretical investigation of conformational states and noncovalent interactions in crystalline sulfonamides with a methoxyphenyl moiety
Brzeski, Jakub,Gawrońska, Ma?gorzata,Kazimierczuk, Katarzyna,Kowalik, Mateusz,Makowski, Mariusz
, p. 6137 - 6162 (2021/09/22)
Four sulfonamide derivatives with a methoxyphenyl moiety, namelyN-{4-[(2-methoxyphenyl)sulfamoyl]phenyl}acetamide (1a),N-{4-[(3-methoxyphenyl)sulfamoyl]phenyl}acetamide (1b), 4-amino-N-(2-methoxyphenyl)benzenesulfonamide (2a) and 4-amino-N-(3-methoxypheny
INHIBITORS OF RAC1 AND USES THEREOF FOR TREATING CANCERS
-
Paragraph 0079-0080, (2019/01/04)
The present invention concerns a compound having the following formula (I): wherein: - A is in particular -N(R'a)-C(=O)-R, R'a being H or a (C1-C6)alkyl group, and R being preferably a group having the following formula (II): - X is in particular chosen from the group consisting of: -SO2-N(R'b)-, R'b being H or a (C1-C6)alkyl group, -N(R"b)-SO2-, R"b being H or a (C1-C6)alkyl group, -CO-NH-, and -NH-CO-, for use for the treatment of cancers, such as metastatic cancers.
Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors
Lawrence, Harshani R.,Kazi, Aslamuzzaman,Luo, Yunting,Kendig, Robert,Ge, Yiyu,Jain, Sanjula,Daniel, Kenyon,Santiago, Daniel,Guida, Wayne C.,Sebti, Said M.
experimental part, p. 5576 - 5592 (2010/09/15)
Screening of the NCI Diversity Set-1 identified PI-083 (NSC-45382) a proteasome inhibitor selective for cancer over normal cells. Focused libraries of novel compounds based on PI-083 chloronaphthoquinone and sulfonamide moieties were synthesized to gain a better understanding of the structure-activity relationship responsible for chymotrypsin-like proteasome inhibitory activity. This led to the demonstration that the chloronaphthoquinone and the sulfonamide moieties are critical for inhibitory activity. The pyridyl group in PI-083 can be replaced with other heterocyclic groups without significant loss of activity. Molecular modeling studies were also performed to explore the detailed interactions of PI-083 and its derivatives with the β5 and β6 subunits of the 20S proteasome. The refined model showed an H-bond interaction between the Asp-114 and the sulfonamide moiety of the PI-083 in the β6 subunit.