Journal article
A Convergent Solid-Phase Synthesis of Actinomycin Analogues - Towards Implementation of Double-Combinatorial Chemistry
The actinomycin antibiotics bind to nucleic acids via both intercalation and hydrogen bonding. We found this 'double-action attack' mechanism very attractive in our search for a novel class of nucleic acid binders. A highly convergent, solid-phase synthetic strategy has been developed for a class of peptide-aryl-peptide conjugates modeled upon natural actinomycins.
The features of this method include the use of Fmoc solid-phase peptide synthesis, side-chain to side-chain cyclization on the solid phase, a chemoselective cleavage step and segment condensation. The synthetic scheme is consistent with the requirements for combinatorial synthesis and furthermore, the final segment condensation allows, for the first time, double-combinatorial chemistry to be performed where two combinatorial libraries can be reacted with each other.
Copyright (C) 1996 Elsevier Science Ltd.
Language: | English |
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Year: | 1996 |
Pages: | 693-698 |
ISSN: | 14643391 and 09680896 |
Types: | Journal article |
DOI: | 10.1016/0968-0896(96)00065-X |
ORCIDs: | 0000-0002-2854-8188 |