50508-66-2Relevant articles and documents
COMPOUNDS HAVING BOTH EFFECTS OF BET BROMODOMAIN PROTEIN INHIBITION AND PD-L1 GENE REGULATION
-
Paragraph 0067-0070, (2022/01/23)
-
Potent Dual BET/HDAC Inhibitors for Efficient Treatment of Pancreatic Cancer
Dong, Guoqiang,He, Shipeng,Li, Yu,Sheng, Chunquan,Wang, Wei,Wu, Shanchao
supporting information, p. 3028 - 3032 (2020/02/11)
As one of the most aggressive and lethal human malignancies with extremely poor prognosis, there is an urgent demand of more effective therapy for the treatment of pancreatic cancer. Reported here is a new, effective therapeutic strategy and the design of small-molecule inhibitors that simultaneously target bromodomain and extra-terminal (BET) and histone deacetylase (HDAC), potentially serving as promising therapeutic agents for pancreatic cancer. A highly potent dual inhibitor (13 a) is identified to possess excellent and balanced activities against BRD4 BD1 (IC50=11 nm) and HDAC1 (IC50=21 nm). Notably, this compound shows higher in vitro and in vivo antitumor potency than the BET inhibitor (+)-JQ1 and the HDAC inhibitor vorinostat, either alone or and in combination, highlighting the advantages of BET/HDAC dual inhibitors for more effective treatment of pancreatic cancer.
PREPARATION OF CONDENSED TRIAZEPINE DERIVATIVES AND THEIR USE AS BET INHIBITORS
-
Paragraph 000118, (2020/01/08)
The invention relates to compounds of the formula: and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of inflammatory diseases, fibtrotic diseases and neoplastic diseases.