51144-70-8Relevant academic research and scientific papers
Reductive Radical Conjugate Addition of Alkyl Electrophiles Catalyzed by a Cobalt/Iridium Photoredox System
Escobar, Randolph A.,Johannes, Jeffrey W.
, p. 6046 - 6051 (2021)
Alkyl and aryl halides have been studied extensively as radical precursors; however, mild and less toxic conditions for the activation of alkyl bromides toward alkyl radicals are still desirable. Reported here is a reductive radical conjugate addition tha
Kinetically guided radical-based synthesis of C(sp3)?C(sp3) linkages on DNA
Wang, Jie,Lundberg, Helena,Asai, Shota,Martín-Acosta, Pedro,Chen, Jason S.,Brown, Stephen,Farrell, William,Dushin, Russell G.,O’Donnell, Christopher J.,Ratnayake, Anokha S.,Richardson, Paul,Liu, Zhiqing,Qin, Tian,Blackmond, Donna G.,Baran, Phil S.
, p. E6404 - E6410 (2018)
DNA-encoded libraries (DEL)-based discovery platforms have re cently been widely adopted in the pharmaceutical industry, mainl due to their powerful diversity and incredible number of mole cules. In the two decades since their disclosure, great strides hav been made to expand the toolbox of reaction modes that are com patible with the idiosyncratic aqueous, dilute, and DNA-sensitiv parameters of this system. However, construction of highly impor tant C(sp3)?C(sp3) linkages on DNA through cross-coupling remain unexplored. In this article, we describe a systematic approach t translating standard organic reactions to a DEL setting throug the tactical combination of kinetic analysis and empirical screenin with information captured from data mining. To exemplify thi model, implementation of the Giese addition to forge high valu C–C bonds on DNA was studied, which represents a radical-base synthesis in DEL.
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors
Rossi, Cristina,Porcelloni, Marina,D'Andrea, Piero,Fincham, Christopher I.,Ettorre, Alessandro,Mauro, Sandro,Squarcia, Antonella,Bigioni, Mario,Parlani, Massimo,Nardelli, Federica,Binaschi, Monica,Maggi, Carlo A.,Fattori, Daniela
, p. 2305 - 2308 (2011/05/15)
We report here the strategy used in our research group to find a new class of histone deacetylase (HDAC) inhibitors. A series of N-substituted 4-alkylpiperazine and 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of HDAC inhibitors (zinc binding moiety-linker-capping group) has been designed, prepared, and tested for HDAC inhibition. Linker length and aromatic capping group connection were systematically varied to find the optimal geometric parameters. A new series of submicromolar inhibitors was thus identified, which showed antiproliferative activity on HCT-116 colon carcinoma cells.
Condensed heterocyclic compounds, their production and use
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, (2008/06/13)
A condensed heterocyclic derivative of the formula (I): STR1 wherein X is an oxygen atom, a sulfur atom or R1 --N1 is a hydrogen atom, a hydrocarbon group which may be substituted or an acyl group which may be substituted; R2 is a hydrogen atom or a hydrocarbon group which may be substituted; ring A is a benzene ring which may be substituted, k is a whole number of 0 to 3; m is a whole number of 1 to 8; and n is a whole number of 1 to 6, or a pharmaceutically acceptable salt thereof exhibiting high colinesterase inhibitory activity, and a method for producing the same.
