Potent double bet / HDAC inhibitors in the treatment of pancreatic cancer

Pancreatic cancer is one of the most aggressive and fatal malignant tumors in human beings The prognosis is very poor, so more effective treatment is urgently needed In order to develop effective new drugs for pancreatic cancer, Wang, from the University of Arizona, USA, recently Wei group proposed a new and effective treatment strategy, that is, using small molecule inhibitors to target both bromine domain and extra terminal domain protein (BET protein) and histone deacetylase (HDAC), researchers designed a series of small molecule drugs reasonably, and screened the most promising drugs for pancreatic cancer treatment Image source: angelw The researchers found that a strong double inhibitor (13a) had good balance activity for brd4bd1 (IC50 = 11nm) and HDAC1 (IC50 = 21nm) It is worth noting that the antitumor activity of the compound in vitro and in vivo is higher than that of bet inhibitor (+) - jq1, HDAC inhibitor vorinostat and their combination, which indicates that this new bet / HDAC double inhibitor has advantages in the treatment of pancreatic cancer, so it is expected to help in the treatment of pancreatic cancer in the future reference material: