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Design and Synthesis of 12‐Aza‐Epothilones (Azathilones)—“Non‐Natural” Natural Products with Potent Anticancer Activity
Author(s) -
Feyen Fabian,
Gertsch Jürg,
Wartmann Markus,
Altmann KarlHeinz
Publication year - 2006
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200601359
Subject(s) - epothilones , natural (archaeology) , chemistry , natural product , combinatorial chemistry , stereochemistry , biology , paleontology
Improving on nature : Azathilones 1 a and 1 b are “non‐natural” natural products derived from epothilones through C→N exchange at position 12. They are highly potent inducers of tubulin polymerization (part of a microtubule is shown in the picture) and inhibit human cancer cell growth in vitro. These compounds present a new structural scaffold for microtubule stabilization and are promising lead structures for anticancer‐drug discovery.