130190-40-8Relevant academic research and scientific papers
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.
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents
Wu, Maojiang,Sun, Qiming,Yang, Chunhao,Chen, Dongdong,Ding, Jian,Chen, Yi,Lin, Liping,Xie, Yuyuan
, p. 869 - 873 (2007/10/03)
A series of 4,5-disubstitute-1,2,3-thiadiazole compounds were designed and synthesized as potent anticancer agents, some of them exhibited excellent in vitro and in vivo inhibitory activity.
REGIOSPECIFICALLY SUBSTITUTED DEOXIBENZOINS BY HORNER CONDENSATION OF AROMATIC ALDEHYDES WITH O-PROTECTED α-ARYL-α-HYDROXYMETHANEPHOSPHONATES
Napolitano, Elio,Ramacciotti, Antonella
, p. 19 - 22 (2007/10/02)
Dimethyl-α-aryl-α-hydroxymethanephosphonates, prepared by addition of dimethyl phosphite to the appropriate aromatic aldehyde, Ar-CHO, have been protected at oxygen by reaction with 3,4-dihydro-2H-pyran catalyzed by p-toluenesulphonic acid and condensed w
