- INHIBITORS OF RAC1 AND USES THEREOF FOR TREATING CANCERS
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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.
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Paragraph 0067-0068
(2019/01/04)
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- INHIBITORS OF RAC1 AND USES THEREOF FOR INDUCING BRONCHODILATATION
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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 pathologies characterized by bronchoconstriction, such as asthma.
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Paragraph 0068; 0069
(2019/01/04)
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- Metal Free Bi(hetero)aryl Synthesis: A Benzyne Truce-Smiles Rearrangement
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A new benzyne transformation is described that affords versatile biaryl structures without recourse to transition-metal catalysis or stoichiometric amounts of organometallic building blocks. Aryl sulfonamides add to benzyne upon fluoride activation, and then undergo an aryl Truce-Smiles rearrangement to afford biaryls with sulfur dioxide extrusion. The reaction proceeds under simple reaction conditions and has excellent scope for the synthesis of sterically hindered atropisomeric biaryl amines. All smiles: Metal-free biaryl synthesis is achieved by adding benzyne to arylsulfonamides. A Smiles rearrangement enables C-C bond formation, thus accessing a variety of functionalized biaryls under mild reaction conditions.
- Holden, Catherine M.,Sohel, Shariar M. A.,Greaney, Michael F.
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supporting information
p. 2450 - 2453
(2016/02/18)
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- Synthesis and biological evaluation of naphthoquinone analogs as a novel class of proteasome inhibitors
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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.
- Lawrence, Harshani R.,Kazi, Aslamuzzaman,Luo, Yunting,Kendig, Robert,Ge, Yiyu,Jain, Sanjula,Daniel, Kenyon,Santiago, Daniel,Guida, Wayne C.,Sebti, Said M.
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experimental part
p. 5576 - 5592
(2010/09/15)
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