Design, synthesis and evaluation of pyrimidinobenzylamide and pyrimidinothiophenamide derivatives as inhibitors of DOT1L and related epigenetic targets DNMT3a, PRMT4 and other HMTs.

• Tác giả: Paola B Arimondo, Christian Bailly, Oscar Omar Castillo-Aguilera, Patrick Depreux, Lenin Domínguez-Ramírez, Laurence Goossens, Sheraz Gul, Ludovic Halby
• Ngôn ngữ: eng
• Ký hiệu phân loại: 272.3 Persecutions of Waldenses and Albigenses
• Thông tin xuất bản: England : RSC medicinal chemistry , 2025
• Bộ sưu tập: NCBI
• ID: 683306

Tóm tắt

The histone methyltransferase DOT1L (DOT1 like, disruptor of telomeric silencing) is responsible for methylation of H3K79, leading to oncogene transcription, and it is involved in the development of different types of cancers such as MLL-rearranged leukemia (MLL-r, myeloid-lymphoid leukemia). Inhibitors of DOT1L have therapeutic potential. Thus, we present herein the