Peng, Xiaopeng; Chen, Jingxuan; Li, Ling; Sun, Zhiqiang; Liu, Jin; Ren, Yichang; Huang, Junli; Chen, Jianjun published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Efficient Synthesis and Bioevaluation of Novel Dual Tubulin/Histone Deacetylase 3 Inhibitors as Potential Anticancer Agents》.Recommanded Product: Methyl 3-bromopropanoate The article contains the following contents:
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. In the experiment, the researchers used Methyl 3-bromopropanoate(cas: 3395-91-3Recommanded Product: Methyl 3-bromopropanoate)
Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Recommanded Product: Methyl 3-bromopropanoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary