131326-23-3Relevant academic research and scientific papers
Compounds and Their Use in Treating Cancer
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Paragraph 0759; 0760, (2019/07/10)
The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, where R1, R4, R5, R6, R7, Linker, X, Y, A, G, D and E have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts and prodrugs thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.
PEPTIDE BOND FORMATION USING AN ENZYME MIMICKING APPROACH
Gennari, Cesare,Molinari, Francesco,Piarulli, Umberto,Bartoletti, Marcella
, p. 7289 - 7300 (2007/10/02)
A man-made enzyme-model based on a concerted proton transfer step (bifunctional catalysis) which mimics the corresponding step in non-ribosomal peptide synthesis was developed.Important features of the model are the following: (a) a bifunctional acid-base catalyst for the thiolester aminolysis rate acceleration, (b) two thiol-containing arms mimicking the "swinging arms" of the enzyme, and (c) symmetry elements so that the process can be iterated with consequent formation of the polypeptide chain.Peptide bond formation was obtained by intramolecularly catalyzed thiolester aminolysis to give 5 in 80percent isolated yield (Scheme IV, V) and with at least a 103-fold rate acceleration in comparison with the corresponding non catalyzed process (4 -> 6)(Scheme IV, Table 1).The reaction is also 4-20 times faster than the analogous process 4 -> 6 run in the presence of 0.1M external catalyst (Et3N-ButCOOH or 2-Pyridone).Important structural and reaction parameters are discussed.A second intramolecular aminolysis reaction gave tripeptide 8 in lower yield (35percent) because of higher steric congestion in the transition state.
