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Design and Total Synthesis of a Superior Family of Epothilone Analogues, which Eliminate Xenograft Tumors to a Nonrelapsable State
Author(s) -
Chou TingChao,
Dong Huajin,
Rivkin Alexey,
Yoshimura Fumihiko,
Gabarda Ana E.,
Cho Young Shin,
Tong William P.,
Danishefsky Samuel J.
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.200352361
Subject(s) - epothilone , chemistry , stereochemistry , cancer research , medicine
Unusually promising profiles of antitumor activity are displayed by 26‐trifluoro‐( E )‐9,10‐dehydro‐dEpoB ( 1 ), the design and practical total synthesis of which is described. This compound promotes tumor shrinkage and disappearance in human xenografts in nude mice at well‐tolerated doses, with complete remission for over two months and early rapid recovery of body weight to the pretreatment control levels.