78573-20-3Relevant academic research and scientific papers
Alkylation of Allyl/Alkenyl Sulfones by Deoxygenation of Alkoxyl Radicals
Han, Jia-Bin,Guo, Ao,Tang, Xiang-Ying
supporting information, p. 2989 - 2994 (2019/02/05)
A challenging deoxygenation of alkoxyl radicals from readily accessible alcohol derivatives was developed, affording facile synthesis of functionalized alkenes with good functional group tolerance under mild reaction conditions. Because alkoxyl radicals can easily undergo β-fragmentations or hydrogen abstractions, this new strategy for deoxygenation of alkoxyl radicals is highly valuable. Moreover, mechanistic studies revealed that the electron-neutral phosphine acts as the deoxygenation reagent.
Structure based optimization of chromen-based TNF-α converting enzyme (TACE) inhibitors on S1′ pocket and their quantitative structure-activity relationship (QSAR) study
Yang, Jee Sun,Chun, Kwangwoo,Park, Jung Eun,Cho, Misun,Seo, Jeongjea,Song, Doona,Yoon, Hongchul,Park, Chun-Ho,Joe, Bo-Young,Choi, Jong-Hee,Kim, Myung-Hwa,Han, Gyoonhee
experimental part, p. 8618 - 8629 (2011/02/25)
A series of coumarin based TACE inhibitors were designed to bind in S1′ pocket of TACE enzyme based on their docking study. Twelve analogues were synthesized and most of compounds were active in vitro TACE enzyme inhibition as well as cellular TNF-α inhibition. Among these, 15l effectively inhibited the production of serum TNF-α by oral administration at a dose of 30 mg/kg. Compound 15l also showed a good oral bioavailability at 42% and effectively inhibited paw edema in rat carrageenan model. Quantitative structure-activity relationship (QSAR) study using genetic function approximation technique (GFA) and docking study were performed to confirm the series of coumarin core TACE inhibitors. QSAR model have been evaluated internally and externally using test set prediction. Through docking study of each molecule, it is validated that the electrostatic descriptors from the QSAR equation could explain the importance of S1′ pocket and the TACE inhibitory activity well.
Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: A structure-activity study
Vassiliou, Stamatia,Mucha, Artur,Cuniasse, Philippe,Georgiadis, Dimitris,Lucet-Levannier, Karine,Beau, Fabrice,Kannan, Rama,Murphy, Gillian,Kn?uper, Vera,Rio, Marie-Christine,Basset, Paul,Yiotakis, Athanasios,Dive, Vincent
, p. 2610 - 2620 (2007/10/03)
Several phosphinic pseudo-tripeptides of general formula R-XaaΨ(PO2- CH2)Xaa'-Yaa'-NH2 were synthesized and evaluated for their in vitro activities to inhibit stromelysin-3, gelatinases A and B, membrane type-1 matrix metalloproteinase, collagenases 1 and 2, and matrilysin. With the exception of collagenase-1 and matrilysin, phosphinic pseudo-tripeptides behave as highly potent inhibitors of matrix metalloproteinases, provided they contain in P1' position an unusual long aryl-alkyl substituent. Study of structure-activity relationships regarding the influence of the R and Xaa' substituents in this series may contribute to the design of inhibitors able to block only a few members of the matrix metalloproteinase family.
Synthesis and Hypoglycemic Activity of Phenylalkyloxiranecarboxylic Acid Derivatives
Eistetter, Klaus,Wolf, Horst P. O.
, p. 109 - 113 (2007/10/02)
A series of new 2-(phenylalkyl)oxirane-2-carboxylic acids has been synthesized and studied for its effects on the concentration of blood glucose.Most of the compounds exhibit remarkable blood glucose lowering activities in fasted rats.Structure-activity s
