The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies》. Authors are Liang, Xuewu; Zang, Jie; Li, Xiaoyang; Tang, Shuai; Huang, Min; Geng, Meiyu; Chou, C. James; Li, Chunpu; Cao, Yichun; Xu, Wenfang; Liu, Hong; Zhang, Yingjie.The article about the compound:Methyl 3-bromopropanoatecas:3395-91-3,SMILESS:O=C(OC)CCBr).Computed Properties of C4H7BrO2. Through the article, more information about this compound (cas:3395-91-3) is conveyed.
Concurrent inhibition of Janus kinase (JAK) and histone deacetylase (HDAC) could potentially improve the efficacy of the HDAC inhibitors in the treatment of cancers and resolve the problem of HDAC inhibitor resistance in some tumors. Here, a novel series of pyrimidin-2-amino-pyrazol hydroxamate derivatives as JAK and HDAC dual inhibitors was designed, synthesized, and evaluated, among which I possessed potent and balanced activities against both JAK2 and HDAC6 with half-maximal inhibitory concentration at the nanomolar level. I exhibited improved antiproliferative and proapoptotic activities over SAHA and ruxolitinib in several hematol. cell lines. Remarkably, I exhibited more potent antiproliferation effect than the combination of SAHA and ruxolitinib in HEL cells bearing JAK2V617F mutation. Pharmacokinetic studies in mice showed that I possessed good bioavailability after i.p. administration. Finally, I showed antitumor efficacy with no significant toxicity in a HEL xenograft model. Collectively, the results confirm the therapeutic potential of JAK and HDAC dual inhibitors in hematol. malignancies and provide valuable leads for further structural optimization and antitumor mechanism study.
This compound(Methyl 3-bromopropanoate)Computed Properties of C4H7BrO2 was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.
Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem