Design, Synthesis, and Biological Properties of Highly Potent Epothilone B Analogues | Zendy

Nicolaou K. C. | Zendy; Sasmal Pradip K. | Zendy; Rassias Gerasimos | Zendy; Reddy Mali Venkat | Zendy; Altmann KarlHeinz | Zendy; Wartmann Markus | Zendy; O'Brate Aurora | Zendy; Giannakakou Paraskevi | Zendy

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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.

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