1197199-79-3Relevant academic research and scientific papers
Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity
Sleebs, Brad E.,Czabotar, Peter E.,Fairbrother, Wayne J.,Fairlie, W. Douglas,Flygare, John A.,Huang, David C. S.,Kersten, Wilhelmus J. A.,Koehler, Michael F. T.,Lessene, Guillaume,Lowes, Kym,Parisot, John P.,Smith, Brian J.,Smith, Morey L.,Souers, Andrew J.,Street, Ian P.,Yang, Hong,Baell, Jonathan B.
, p. 1914 - 1926 (2011/05/30)
ABT-737 and ABT-263 are potent inhibitors of the BH3 antiapoptotic proteins, Bcl-xL and Bcl-2. This class of putative anticancer agents invariantly contains an acylsulfonamide core. We have designed and synthesized a series of novel quinazoline-based inhibitors of Bcl-2 and Bcl-xL that contain a heterocyclic alternative to the acylsulfonamide. These compounds exhibit submicromolar, mechanism-based activity in human small-cell lung carcinoma cell lines in the presence of 10% human serum. This comprises the first successful demonstration of a quinazoline sulfonamide core serving as an effective benzoylsulfonamide bioisostere. Additionally, these novel quinazolines comprise only the second known class of Bcl-2 family protein inhibitors to induce mechanism-based cell death.
ARYLSULFONAMIDE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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, (2009/12/27)
Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti apoptotic protein family member.
