172846-56-9Relevant articles and documents
Modular Solid-Phase Synthesis of Antiprotozoal Barnesin Derivatives
Roman, Dávid,Ragu?, Luka,Keiff, Fran?ois,Meyer, Florian,Barthels, Fabian,Schirmeister, Tanja,Kloss, Florian,Beemelmanns, Christine
, p. 3744 - 3748 (2020)
Here, we applied and optimized a solid support (SP)-based Horner-Wadsworth-Emmons reagent to prepare SP-bound vinylogous amino acids. Subsequent SP-based peptide synthesis, global deprotection, and chemical modifications yielded 14 lipodipeptides carrying
Backbone thioamide directed macrocyclisation: Lactam stapling of peptides
Hutton, Craig A.,Taresh, Ameer B.
supporting information, p. 1488 - 1492 (2022/03/01)
A novel method for lactam stapling of Asp/Lys-containing peptides has been developed that does not require coupling agents. A backbone thioamide is incorporated at the N-terminal side of the aspartate residue. Ag(i)-promoted activation of the thioamide in the vicinity of the Asp carboxylate generates a cyclic isoimide intermediate that is trapped by the Lys amine to generate the macrolactam. This method is suitable for generation of i,i+2, i,i+3, and i,i+4-spaced lactam-bridged peptides. This journal is
NEW TARGETED CYTOTOXIC RATJADONE DERIVATIVES AND CONJUGATES THEREOF
-
Paragraph 00206; 00207, (2019/02/25)
The present invention is directed to novel natural product-derived ratjadone-based compounds useful as payloads (or toxins) in drug-conjugates constructs with cell target binding moieties (CTBM) and payload-linker compounds useful in connection with drug conjugates. The present invention further relates to new ratjadone compositions including the aforementioned payloads, payload-linkers and drug conjugates, and methods for using these payloads, payload-linkers and drug conjugates, to treat pathological conditions including cancer, inflammatory and infectious diseases.