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Design, Synthesis, and Biological Properties of Highly Potent Epothilone B Analogues
Author(s) -
Nicolaou K. C.,
Sasmal Pradip K.,
Rassias Gerasimos,
Reddy Mali Venkat,
Altmann KarlHeinz,
Wartmann Markus,
O'Brate Aurora,
Giannakakou Paraskevi
Publication year - 2003
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.200351819
Subject(s) - cyclopropane , epothilone , stereochemistry , epoxide , potency , chemistry , biological activity , ring (chemistry) , cancer cell lines , epothilones , combinatorial chemistry , in vitro , biochemistry , cancer , biology , cancer cell , organic chemistry , genetics , catalysis
A number of rationally designed epoxide and cyclopropane epothilone B ( 1 ) analogues with substituted side chains were prepared and their biological activities were evaluated against a series of human cancer cell lines. The cyclopropane analogue 2 with a methylsulfanylthiazole ring stands out as the most potent compound and is sixfold more active than 1 . The methylsulfanyl group enhances the potency of these compounds.