The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: Methyl 3-bromopropanoate(SMILESS: O=C(OC)CCBr,cas:3395-91-3) is researched.Category: quinuclidine. The article 《Efficient Synthesis and Bioevaluation of Novel Dual Tubulin/Histone Deacetylase 3 Inhibitors as Potential Anticancer Agents》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:3395-91-3).
Novel dual HDAC3/tubulin inhibitors were designed and efficiently synthesized by combining the pharmacophores of SMART (tubulin inhibitor) and MS-275 (HDAC inhibitor), among which compound 15c was found to be the most potent and balanced HDAC3/tubulin dual inhibitor with high HDAC3 activity (IC50 = 30 nM) and selectivity (SI > 1000) as well as excellent antiproliferative potency against various cancer cell lines, including an HDAC-resistant gastric cancer cell line (YCC3/7) with IC50 values in the range of 30-144 nM. Compound 15c inhibited B16-F10 cancer cell migration and colony formation. In addition, 15c demonstrated significant in vivo antitumor efficacy in a B16-F10 melanoma tumor model with a better TGI (70.00%, 10 mg/kg) than that of the combination of MS-275 and SMART. Finally, 15c presented a safe cardiotoxicity profile and did not cause nephro-/hepatotoxicity. Collectively, this work shows that compound 15c represents a novel tubulin/HDAC3 dual-targeting agent deserving further investigation as a potential anticancer agent.
There is still a lot of research devoted to this compound(SMILES：O=C(OC)CCBr)Recommanded Product: Methyl 3-bromopropanoate, and with the development of science, more effects of this compound(3395-91-3) can be discovered.
Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem