478964-96-4Relevant articles and documents
Base-Catalyzed, Solvent-Free Synthesis of Rigid V-Shaped Epoxydibenzo[b,f][1,5]diazocines
Bisek, Bartosz,Górecki, Marcin,Michalak, Micha?,Nowacki, Micha?
, p. 8955 - 8969 (2021)
A novel method for the synthesis of epoxydibenzo[b,f][1,5]diazocines exhibiting a V-shaped molecular architecture is reported. The unique approach is based on unprecedented base-catalyzed, solvent-free autocondensation and cross-condensation of fluorinate
Synthesis and biological evaluation of novel quinazoline-triazole hybrid compounds with potential use in Alzheimer's disease
Dang Thi, Tuyet Anh,Le-Nhat-Thuy, Giang,Nguyen Hoang, Sa,Nguyen Thi, Huong,Nguyen Thi, Nga,Nguyen Thi, Thu Ha,Nguyen, Tuyen Van,Pham-The, Hai
supporting information, (2020/07/23)
A library of twelve quinazoline-triazole hybrid compounds were designed, synthesized and evaluated as a novel class of acetylcholinesterase inhibitors to treat Alzheimer's disease (AD). The biological assay results demonstrated the ability of several hybrid compounds to inhibit AChE enzyme (IC50 range = 0.2–83.9 μM). To understand the high potential activity of these compounds, molecular docking simulations were performed to get better insights into the mechanism of binding of quinazoline-triazole hybrid compounds. As expected, compounds 8a and 9a-b bind to both catalytic anionic site (CAS) and peripheral anionic site (PAS) in the active site of AChE enzyme, which implicates that these compounds could act as dual binding site inhibitors. These compounds were not cytotoxic and they also displayed appropriated physicochemical as well as pharmacokinetic profile to be developed as novel anti-AD drug candidates.
Photo-triggered release of caged camptothecin prodrugs from dually responsive shell cross-linked micelles
Hu, Xianglong,Tian, Jie,Liu, Tao,Zhang, Guoying,Liu, Shiyong
, p. 6243 - 6256 (2013/09/02)
We report on the fabrication of dynamic covalent shell cross-linked (SCL) micelles with hydrophobic cores conjugated with photocaged chemotherapeutic drugs and coronas functionalized with ligands for tumor cell targeting. Two types of amphiphilic diblock