2746-25-0Relevant articles and documents
Discovery of substituted 1,4-dihydroquinolines as novel promising class of P-glycoprotein inhibitors: First structure-activity relationships and bioanalytical studies
Hemmer, Marc,Krawczyk, S?ren,Simon, Ina,Hilgeroth, Andreas
, p. 3005 - 3008 (2015)
Multidrug resistance (mdr) is the most important problem in the therapeutical treatment of cancer. One central problem in the resistance proceeding is the expression of transmembrane efflux pumps which transport drugs out of the cells. We developed novel substituted 1,4-dihydroquinolines as inhibitors of the transmembrane efflux pump P-glycoprotein. Structure-activity relationships are discussed for this first series. Promising active inhibitors have been identified and first bioanalytical studies have been carried out to address questions of cellular toxicity, P-gp substrate as well as mdr reversal properties.
Design, synthesis, and structure–activity relationship study of potent mapk11 inhibitors
Gong, Mengdie,Li, Honglin,Li, Lu,Li, Shiliang,Sun, Hongxia,Tu, Mingyan,Zhao, Zhenjiang,Zhu, Lili
supporting information, (2022/01/04)
Huntington’s disease (HD) is a rare single-gene neurodegenerative disease, which can only be treated symptomatically. Currently, there are no approved drugs for HD on the market. Studies have found that MAPK11 can serve as a potential therapeutic target f
Deconjugative α-Alkylation of Cyclohexenecarboxaldehydes: An Access to Diverse Terpenoids
Chahboun, Rachid,Botubol-Ares, José Manuel,Durán-Pe?a, María Jesús,Jiménez, Fermín,Alvarez-Manzaneda, Ramón,Alvarez-Manzaneda, Enrique
, p. 8742 - 8754 (2021/07/19)
A general and efficient method for the deconjugative α-alkylation of α,β-unsaturated aldehydes promoted by a synergistic effect between tBuOK and NaH, which considerably increases the reaction rate under mild conditions, is reported. The β,γ-unsaturated aldehyde, resulting from the α-alkylation, is transformed in high yield into the corresponding allyl acetate via a lead(IV) acetate-mediated oxidative fragmentation. This strategy could be used for the construction of the carbon skeleton of a wide variety of alkyl or arylterpenoids.
Readily Reconfigurable Continuous-Stirred Tank Photochemical Reactor Platform
Blacker, A. John,Francis, Daniel,Kapur, Nikil,Marsden, Stephen P.
supporting information, (2022/01/12)
A new modular photochemical continuous stirred-tank reactor (CSTR) design is described, based upon the development of light-source units that can be fitted to the previously described fReactor CSTR platform. In addition to use in homogeneous photochemical reactions (e.g., photoredox-catalyzed hydroamination), these units are especially well suited to handling multiphasic mixtures, exemplified here in solid-liquid (Wohl-Ziegler bromination) and gas-liquid (photocatalytic oxidative decarboxylation) reactions. The use of slurries as input feeds allows for the intensification of photochemical brominations, while the modular nature of the system facilitates the simple integration of downstream reaction steps, exemplified here in a continuous synthesis of an intermediate for the antihypertensive drug valsartan.