850133-84-5Relevant academic research and scientific papers
A detour route for meta functionalization of phenols
Chittimalla, Santhosh Kumar,Kuppusamy, Rajesh,Bandi, Chennakesavulu
, p. 1991 - 1996 (2014)
Cyclohexadienones participate in a two-step procedure, a Michael addition followed by aromatization, providing hitherto difficult-to-synthesize meta-functionalized phenol derivatives in good yield. Application of the developed approach is exemplified by synthesizing C-aryl acetophenones, C-aryl glycines, and elemicin - an allylphenol natural product. Georg Thieme Verlag Stuttgart · New York.
Novel diaryl-2H-azirines: Antitumor hybrids for dual-targeting tubulin and DNA
Lin, Shibo,Liang, Yuru,Cheng, Jiayi,Pan, Feng,Wang, Yang
, (2021/02/16)
Multiple-target drugs may achieve better therapeutic effect via different pathways than single-target ones, especially for complex diseases. Tubulin and DNA are well-characterized molecular targets for anti-cancer drug development. A novel class of diaryl substituted 2H-azirines were designed based on combination of pharmacophores from Combretastatin A-4 (CA-4) and aziridine-type alkylating agents, which are known tubulin polymerization inhibitor and DNA damaging agents, respectively. The antitumor activities of these compounds were evaluated in vitro and 6h showed the most potent activities against four cancer cell lines with IC50 values ranging from 0.16 to 1.40 μM. Further mechanistic studies revealed that 6h worked as a bifunctional agent targeting both tubulin and DNA. In the nude mice xenograft model, 6h significantly inhibited the tumor growth with low toxicity, demonstrating the promising potential for further developing novel cancer therapy with a unique mechanism.
