Category: bromides-buliding-blocksIn 2019 ,《Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer Therapy》 appeared in Journal of Medicinal Chemistry. The author of the article were Chen, Yong; Yuan, Xue; Zhang, Wanhua; Tang, Minghai; Zheng, Li; Wang, Fang; Yan, Wei; Yang, Shengyong; Wei, Yuquan; He, Jun; Chen, Lijuan. The article conveys some information:
In the present study, a series of novel dual-target histone deacetylase (HDAC) and mammalian target of rapamycin (mTOR) inhibitors were designed and synthesized using pyrimidine-pyrazolyl pharmacophore to append HDAC recognition cap and hydroxamic acid as a zinc-binding motif. Among them, I was the optimal lead compound with potent inhibition activities against mTOR and HDAC1 with half-maximal inhibitory concentration of 1.2 and 0.19 nM, resp. Western blot confirmed that I could upregulate acetylation of H3 and α-tubulin and downregulate mTOR-related downstream mediators. I could also stimulate cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis. I showed comparable antitumor activity with the combination medication in MM1S xenograft model with a tumor growth inhibitory rate of 72.5%, without causing significant loss of body weight and toxicity. All of the results indicated that I could be a promising dual target inhibitor for treating hematol. malignancies. The experimental process involved the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Category: bromides-buliding-blocks)
Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. In contrast, terrestrial plants account only for a few bromine-containing compounds.Category: bromides-buliding-blocks
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary