226070-69-5Relevant articles and documents
CHEMOKINE CXCR4 RECEPTOR MODULATORS AND USES RELATED THERETO
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Page/Page column 173; 174; 175, (2018/09/19)
The disclosure relates to chemokine CXCR4 receptor modulators and uses related thereto. The receptor modulators can be formulated to form pharmaceutical compositions comprising the disclosed compounds or pharmaceutically acceptable salts or prodrugs thereof. The compositions may be used for managing CXCR4 related conditions, typically prevention or treatment of viral infections abnormal cellular proliferation, retinal degeneration, inflammatory diseases, or as an immunostimulant or immunosuppressant or for managing cancer and may be administered with another active ingredient such as an antiviral agent or chemotherapeutic agent.
Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists
Procopiou, Panayiotis A.,Barrett, John W.,Barton, Nicholas P.,Begg, Malcolm,Clapham, David,Copley, Royston C. B.,Ford, Alison J.,Graves, Rebecca H.,Hall, David A.,Hancock, Ashley P.,Hill, Alan P.,Hobbs, Heather,Hodgson, Simon T.,Jumeaux, Coline,Lacroix, Yannick M. L.,Miah, Afjal H.,Morriss, Karen M. L.,Needham, Deborah,Sheriff, Emma B.,Slack, Robert J.,Smith, Claire E.,Sollis, Steven L.,Staton, Hugo
supporting information, p. 1946 - 1960 (2013/05/09)
A series of indazole arylsulfonamides were synthesized and examined as human CCR4 antagonists. Methoxy- or hydroxyl- containing groups were the more potent indazole C4 substituents. Only small groups were tolerated at C5, C6, or C7, with the C6 analogues being preferred. The most potent N3-substituent was 5-chlorothiophene-2-sulfonamide. N1 meta-substituted benzyl groups possessing an α-amino-3-[(methylamino)acyl]- group were the most potent N1-substituents. Strongly basic amino groups had low oral absorption in vivo. Less basic analogues, such as morpholines, had good oral absorption; however, they also had high clearance. The most potent compound with high absorption in two species was analogue 6 (GSK2239633A), which was selected for further development. Aryl sulfonamide antagonists bind to CCR4 at an intracellular allosteric site denoted site II. X-ray diffraction studies on two indazole sulfonamide fragments suggested the presence of an important intramolecular interaction in the active conformation.
HISTONE DEACETYLASE INHIBITORS
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, (2011/04/13)
The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.
