The present application is directed to the use of substituted 2-phenyl-3H-quinazolin-4-ones and analogs for inhibiting BET (bromodomain and extra terminal domain) 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.La présente invention concerne des composés de polyphénol d'origine non naturelle qui inhibent les protéines à bromodomaine et à domaine extra-terminal (BET). Les compositions et procédés décrits peuvent être utilisés pour traiter et prévenir des maladies ou des pathologies qui sont sensibles à l'administration d'un inhibiteur de BET.