4-Demethoxy-3'-N-trifluoroacetyldoxorubicin. Synthesis and solid tumor activity

D. Horton; W. Priebe; J. P. Carter; J. Filppi; R. L. Wolgemuth

4-Demethoxy-3'-N-trifluoroacetyldoxorubicin. Synthesis and solid tumor activity

D. Horton, W. Priebe, J. P. Carter, J. Filppi, R. L. Wolgemuth

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

Abstract

A new route has been developed for the preparation of 3'-N-protected doxorubicin analogues. 4-Demethoxy-3'-N-trifluoroacetyldoxorubicin (5) was synthesized in an approach to an orally active anthracycline analogue. Tested against the B-16 murine solid tumor in mice, this compound increased life span by 133% when it was administered intraperitoneally at 25 mg/kg, and 52% when it was given orally at 50 mg/kg.

Original language	English (US)
Pages (from-to)	123-129
Number of pages	7
Journal	Drug Design and Delivery
Volume	6
Issue number	2
State	Published - 1990
Externally published	Yes

Keywords

Anti-tumor agents
Doxorubicin

ASJC Scopus subject areas

Molecular Medicine
Pharmacology
Drug Discovery

Cite this

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year = "1990",

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AU - Horton, D.

AU - Priebe, W.

AU - Carter, J. P.

AU - Filppi, J.

AU - Wolgemuth, R. L.

PY - 1990

Y1 - 1990

N2 - A new route has been developed for the preparation of 3'-N-protected doxorubicin analogues. 4-Demethoxy-3'-N-trifluoroacetyldoxorubicin (5) was synthesized in an approach to an orally active anthracycline analogue. Tested against the B-16 murine solid tumor in mice, this compound increased life span by 133% when it was administered intraperitoneally at 25 mg/kg, and 52% when it was given orally at 50 mg/kg.

AB - A new route has been developed for the preparation of 3'-N-protected doxorubicin analogues. 4-Demethoxy-3'-N-trifluoroacetyldoxorubicin (5) was synthesized in an approach to an orally active anthracycline analogue. Tested against the B-16 murine solid tumor in mice, this compound increased life span by 133% when it was administered intraperitoneally at 25 mg/kg, and 52% when it was given orally at 50 mg/kg.

KW - Anti-tumor agents

KW - Doxorubicin

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IS - 2

ER -

4-Demethoxy-3'-N-trifluoroacetyldoxorubicin. Synthesis and solid tumor activity

Abstract

Keywords

ASJC Scopus subject areas

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