294860-95-0Relevant academic research and scientific papers
A Modular Synthesis of Teraryl-Based α-Helix Mimetics, Part 3: Iodophenyltriflate Core Fragments Featuring Side Chains of Proteinogenic Amino Acids
Breinbauer, Rolf,Dobrounig, Patrick,Doler, Carina,Holzinger, Ella B.,Schreiner, Till,Steinegger, Andreas,Trobe, Melanie,Vareka, Martin
, (2022/03/02)
Teraryl-based α-helix mimetics have proven to be useful compounds for the inhibition of protein-protein interactions (PPI). We have developed a modular and flexible approach for the synthesis of teraryl-based α-helix mimetics using a benzene core unit featuring two leaving groups of differentiated reactivity in the Pd-catalyzed cross-coupling used for teraryl assembly. In previous publications we have introduced the methodology of 4-iodophenyltriflates decorated with the side chains of some of the proteinogenic amino acids. We herein report the core fragments corresponding to the previously missing amino acids Arg, Asn, Asp, Met, Trp and Tyr. Therefore, our set now encompasses all relevant amino acid analogues with the exception of His. In order to be compatible with the triflate moiety, some of the nucleophilic side chains had to be provided in a protected form to serve as stable building blocks. Additionally, cross-coupling procedures for the assembly of teraryls were investigated.
Gamma-ketoacid dipeptide derivatives as inhibitors of caspase-3
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, (2008/06/13)
This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods for treatment of caspase-3 mediated diseases.
Gamma-ketoacid dipeptides as inhibitors of caspase-3
-
, (2008/06/13)
This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods for treatment of caspase-3 mediated diseases.
Gamma-ketoacid dipeptides as inhibitors of caspase-3
-
, (2008/06/13)
Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is impl
