Synthetic Route of C9H9BrO2In 2020 ,《Discovery of Thieno[2,3-d]pyrimidine-Based Hydroxamic Acid Derivatives as Bromodomain-Containing Protein 4/Histone Deacetylase Dual Inhibitors Induce Autophagic Cell Death in Colorectal Carcinoma Cells》 was published in Journal of Medicinal Chemistry. The article was written by Pan, Zhaoping; Li, Xiang; Wang, Yujia; Jiang, Qinglin; Jiang, Li; Zhang, Min; Zhang, Nan; Wu, Fengbo; Liu, Bo; He, Gu. The article contains the following contents:
Bromodomain-containing protein 4 (BRD4) and histone deacetylases (HDAC) are both attractive epigenetic targets in cancer and other chronic diseases. Based on the integrated fragment-based drug design, synthesis, and in vitro and in vivo evaluations, a series of novel thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives are discovered as selective BRD4-HDAC dual inhibitors. Compound 17c is the most potent inhibitor for BRD4 and HDAC with IC50 values at nanomolar levels, as well as the expression level of c-Myc, and increases the acetylation of histone H3. Moreover, 17c presents inhibitory effects on the proliferation of colorectal carcinoma (CRC) cells via inducing autophagic cell death. It also has a good pharmacokinetic profile in rats and oral bioavailability of 40.5%. In the HCT-116 xenograft in vivo models, 17c displays potent inhibitory efficiency on tumor growth by inducing autophagic cell death and suppressing IL6-JAK-STAT signaling pathways. Our results suggest that the BRD4-HDAC dual inhibition might be an attractive therapeutic strategy for CRC. The results came from multiple reactions, including the reaction of Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Synthetic Route of C9H9BrO2)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Synthetic Route of C9H9BrO2 The most pervasive is the naturally produced bromomethane.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary