Xu, Xi; Zhang, Di; Zhao, Tengteng; Wang, Min; Li, Yu; Du, Qianming; Kou, Junping; Li, Zhiyu; Bian, Jinlei published an article in 2022. The article was titled 《Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation》, and you may find the article in European Journal of Medicinal Chemistry.Related Products of 76006-33-2 The information in the text is summarized as follows:
A series of novel biphenyl-based scaffold derivatives were identified as selective histone deacetylase 6 (HDAC6) inhibitors through an inhouse compound library screening approach. The biol. evaluation indicated that most of target compounds exhibited moderate to good inhibitory activity and selectivity against HDAC6. Especially, compound C10 was identified as a potent and highly selective HDACs inhibitor, with HDAC1 IC50 value of 3600 nM, HDAC6 IC50 value of 23 nM, and the HDAC1/6 selectivity index of 157. Moreover, C10 displayed robust anti-proliferative activity, induced cancer cells apoptosis, increased the level of acetylated α-tubulin and inhibited cancer cells migration in vitro. C10 showed significant antitumor efficacy (TGI: 75%) in CT26 colon carcinoma xenograft model in mice with no considerable toxicity in vivo. More importantly, C10 could also activate antitumor immunity so as to synergistically exert antitumor effects in vivo. Overall, our findings have provided a new avenue for design, development and investigation into the mechanism underlying the antitumor efficacy of selective HDAC6 inhibitors. The experimental part of the paper was very detailed, including the reaction process of 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Related Products of 76006-33-2)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Related Products of 76006-33-2 Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary