《Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide》 was written by Zhang, Fangqing; Wu, Zhenwei; Chen, Pan; Zhang, Jian; Wang, Tao; Zhou, Jinpei; Zhang, Huibin. Safety of Ethyl 5-bromovalerate And the article was included in Bioorganic & Medicinal Chemistry in 2020. The article conveys some information:
Synthesis of dihydroquinazolinone-lenalidomide/pomalidomide derivatives I [n=1,2,3,4,5,6], II [n=4,5,6] and III [X = CH2, CO; n=0,1,2,3] and biol. evaluation of PROTAC BRD4 degraders was discovered. Gratifyingly, several compounds showed excellent inhibitory activity against BRD4 and high anti-proliferative potency against human monocyte lymphoma cell line THP-1. Especially, compound III [X = CO; n=0] (BRD4 BD1, IC50 = 41.8 nM) achieved a submicromolar IC50 value of 0.81μM in inhibiting the growth of THP-1 cell line, and was 4 times more potent than compound IV. Moreover, the mechanism study established that III [X = CO; n=0] could effectively induced the degradation of BRD4 protein and suppression of c-Myc. The experimental process involved the reaction of 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