In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies, published in 2019-04-25, which mentions a compound: 3395-91-3, mainly applied to pyrimidinaminopyrazole hydroxamate preparation JAK HDAC inhibitor hematol malignancy treatment; selected pyrimidinaminopyrazole compound pharmacokinetic study bioavailability antitumor efficacy, HPLC of Formula: 3395-91-3.
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 some applications, this compound(3395-91-3)HPLC of Formula: 3395-91-3 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.
Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem