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USE OF SUBSTITUTED 2-PHENYL-3H-QUINAZOLIN-4-ONES AND ANALOGS FOR INHIBITING BROMODOMAIN AND EXTRA TERMINAL DOMAIN (BET) PROTEINS
USE OF SUBSTITUTED 2-PHENYL-3H-QUINAZOLIN-4-ONES AND ANALOGS FOR INHIBITING BROMODOMAIN AND EXTRA TERMINAL DOMAIN (BET) PROTEINS
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机译:使用取代的2-苯基-3H-喹那啉-4-酮和类似物来抑制溴代和外部末端域(BET)蛋白
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摘要
The present application is directed to the use of substituted 2-phenyl-3H-quinazolin-4-ones and analogs for inhibiting bromodomain and extra terminal domain (BET) proteins. The disclosed compounds can be used for the treatment of cancers that exhibit c-myc overexpression, cancers that overexpress n-myc, and cancers that rely on the recruitment of p-TEFb to regulate activated oncogenes, such as Burkitt's lymphoma, acute myelogenous leukemia, multiple myeloma, aggressive human medulloblastoma, hematological, epithelial cancers, lung cancers, breast cancers, colon carcinomas, midline carcinomas, mesenchymal tumors, hepatic tumors, renal tumors and neurological tumors.
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