66415-01-8Relevant articles and documents
Design criteria for minimalist mimics of protein-protein interface segments
Taechalertpaisarn, Jaru,Lyu, Rui-Liang,Arancillo, Maritess,Lin, Chen-Ming,Jiang, Zhengyang,Perez, Lisa M.,Ioerger, Thomas R.,Burgess, Kevin
supporting information, p. 908 - 915 (2019/01/30)
Small molecules that can interrupt or inhibit protein-protein interactions (PPIs) are valuable as probes in chemical biology and medicinal chemistry, but they are also notoriously difficult to develop. Design of non-peptidic small molecules that mimic ami
Total synthesis and biological evaluation of tamandarin B analogues
Adrio, Javier,Cuevas, Carmen,Manzanares, Ignacio,Joullie, Madeleine M.
, p. 5129 - 5138 (2008/02/07)
(Chemical Equation Presented) Tamandarins A and B are a class of marine natural cyclodepsipeptides with structures and biological activities closely related to those of the didemnins. The easier synthetic access to tamandarins accelerates the preparation of new macrocyclic derivatives of this family of antitumor, antiviral, and immunosuppressive compounds. The optimization of the previously reported synthetic route to tamandarins by changing the macrolactamization site from Nst1 and Thr6 to Pro 4 and N,O-Me2Tyr5 residues led to a significant improvement in the reaction yield. Using this new synthetic approach, four new macrocyclic analogues of tamandarin B were prepared and evaluated for anticancer activity. These results provide further insight into the structure-activity relationship of the tamandarins and didemnins.
Application of a unique automated synthesis system for solution-phase peptide synthesis
Sugawara,Kobayashi,Okamoto,Kitada,Fujino
, p. 1272 - 1280 (2007/10/02)
An automated synthesis system, which is suitable for repetitive syntheses using similar reaction procedures, was used to synthesize systematically a library of all possible dipeptides (25) and tripeptides (125) from 5 protected amino acids. The apparatus has also been applied to the automated synthesis of 10 fragment tripeptide derivatives that are constituents of the hormone PACAP-27. The measured molecular optical rotation values of the library of 125 tripeptides were found to correlate well with calculated values obtained by summation of the molecular optical rotation values for the constituent amino acids.