The author of 《Oxazole-bridged combretastatin A-4 derivatives with tethered hydroxamic acids: structure-activity relations of new inhibitors of HDAC and/or tubulin function》 were Schmitt, Florian; Gosch, Lisa Chiara; Dittmer, Alexandra; Rothemund, Matthias; Mueller, Thomas; Schobert, Rainer; Biersack, Bernhard; Volkamer, Andrea; Hoepfner, Michael. And the article was published in International Journal of Molecular Sciences in 2019. Safety of Ethyl 5-bromovalerate The author mentioned the following in the article:
New inhibitors of tubulin polymerization and/or histone deacetylase (HDAC) activity were synthesized by attaching alkyl tethered hydroxamic acid appendages of varying length to oxazole-bridged combretastatin A-4 analogous caps. While their antiproliferative and microtubule disrupting effect was most pronounced for derivatives with short spacers, HDAC inhibition was strongest for those with longer spacers. These findings were further supported by computational methods such as structure-based docking experiments exploring the target interactions of the derivatives with varying linkers. For instance, compounds featuring short four-atom spacers between cap and hydroxamic acid inhibited the growth of various cancer cell lines and human endothelial hybrid cells with IC50 values in the low nanomolar range. In line with their ability to inhibit the microtubule assembly, four- and five-atom spacered hydroxamic acids caused an accumulation of 518A2 melanoma cells in G2/M phase, whereas a compound featuring a six-atom spacer and performing best in HDAC inhibition, induced a G1 arrest in these cells. All these beneficial anticancer activities together with their selectivity for cancer cells over non-malignant cells, point out the great potential of these novel pleiotropic HDAC and tubulin inhibitors as drug candidates for cancer therapy. In the part of experimental materials, we found many familiar compounds, such as Ethyl 5-bromovalerate(cas: 14660-52-7Safety of Ethyl 5-bromovalerate)
Ethyl 5-bromovalerate(cas: 14660-52-7) 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.Safety of Ethyl 5-bromovalerate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary