Design and Total Synthesis of a Superior Family of Epothilone Analogues, which Eliminate Xenograft Tumors to a Nonrelapsable State

Ting Chao Chou; Huajin Dong; Alexey Rivkin; Fumihiko Yoshimura; Ana E. Gabarda; Young Shin Cho; William P. Tong; Samuel J. Danishefsky

doi:10.1002/anie.200352361

Design and Total Synthesis of a Superior Family of Epothilone Analogues, which Eliminate Xenograft Tumors to a Nonrelapsable State

Ting Chao Chou, Huajin Dong, Alexey Rivkin, Fumihiko Yoshimura, Ana E. Gabarda, Young Shin Cho, William P. Tong, Samuel J. Danishefsky

Cancer Systems Imaging

Research output: Contribution to journal › Article › peer-review

72 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	4762-4767
Number of pages	6
Journal	Angewandte Chemie - International Edition
Volume	42
Issue number	39
DOIs	https://doi.org/10.1002/anie.200352361
State	Published - Oct 13 2003

Keywords

Antitumor agents
Conformation analysis
Epothilones
Natural products
Structure-activity relationships

ASJC Scopus subject areas

Catalysis
General Chemistry

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title = "Design and Total Synthesis of a Superior Family of Epothilone Analogues, which Eliminate Xenograft Tumors to a Nonrelapsable State",

abstract = "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.",

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author = "Chou, {Ting Chao} and Huajin Dong and Alexey Rivkin and Fumihiko Yoshimura and Gabarda, {Ana E.} and Cho, {Young Shin} and Tong, {William P.} and Danishefsky, {Samuel J.}",

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AU - Chou, Ting Chao

AU - Dong, Huajin

AU - Rivkin, Alexey

AU - Yoshimura, Fumihiko

AU - Gabarda, Ana E.

AU - Cho, Young Shin

AU - Tong, William P.

AU - Danishefsky, Samuel J.

PY - 2003/10/13

Y1 - 2003/10/13

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AB - 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.

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KW - Conformation analysis

KW - Epothilones

KW - Natural products

KW - Structure-activity relationships

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Design and Total Synthesis of a Superior Family of Epothilone Analogues, which Eliminate Xenograft Tumors to a Nonrelapsable State

Abstract

Keywords

ASJC Scopus subject areas

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