Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 3395-91-3, is researched, Molecular C4H7BrO2, about Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies, the main research direction is pyrimidinaminopyrazole hydroxamate preparation JAK HDAC inhibitor hematol malignancy treatment; selected pyrimidinaminopyrazole compound pharmacokinetic study bioavailability antitumor efficacy.Electric Literature of C4H7BrO2.
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.
In addition to the literature in the link below, there is a lot of literature about this compound(Methyl 3-bromopropanoate)Electric Literature of C4H7BrO2, illustrating the importance and wide applicability of this compound(3395-91-3).
Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem