Characterization of the taxol structure-activity profile for the locus of the A-ring side chain

Charles S. Swindell; Julia M. Heerding; Nancy E. Krauss; Susan B. Horwitz; Israel Ringel

doi:10.1016/S0960-894X(01)80527-8

Characterization of the taxol structure-activity profile for the locus of the A-ring side chain

Charles S. Swindell, Julia M. Heerding, Nancy E. Krauss, Susan B. Horwitz, Israel Ringel

Molecular Pharmacology

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

12 Scopus citations

Abstract

Two series of taxol analogs with various N-acyl groups on 3′-phenylisoserine and isoserine A-ring side chains, respectively, were prepared, and their microtubule assembly acitivities and cytotoxicities toward J774.2 cells were evaluated. Biological activities were adversely affected by the structural modifications investigated, although the 3′-phenylisoserine series was significantly more active than the isoserine series.

Original language	English (US)
Pages (from-to)	1531-1536
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	4
Issue number	12
DOIs	https://doi.org/10.1016/S0960-894X(01)80527-8
State	Published - Jun 23 1994

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)80527-8

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abstract = "Two series of taxol analogs with various N-acyl groups on 3′-phenylisoserine and isoserine A-ring side chains, respectively, were prepared, and their microtubule assembly acitivities and cytotoxicities toward J774.2 cells were evaluated. Biological activities were adversely affected by the structural modifications investigated, although the 3′-phenylisoserine series was significantly more active than the isoserine series.",

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AU - Swindell, Charles S.

AU - Heerding, Julia M.

AU - Krauss, Nancy E.

AU - Horwitz, Susan B.

AU - Ringel, Israel

PY - 1994/6/23

Y1 - 1994/6/23

N2 - Two series of taxol analogs with various N-acyl groups on 3′-phenylisoserine and isoserine A-ring side chains, respectively, were prepared, and their microtubule assembly acitivities and cytotoxicities toward J774.2 cells were evaluated. Biological activities were adversely affected by the structural modifications investigated, although the 3′-phenylisoserine series was significantly more active than the isoserine series.

AB - Two series of taxol analogs with various N-acyl groups on 3′-phenylisoserine and isoserine A-ring side chains, respectively, were prepared, and their microtubule assembly acitivities and cytotoxicities toward J774.2 cells were evaluated. Biological activities were adversely affected by the structural modifications investigated, although the 3′-phenylisoserine series was significantly more active than the isoserine series.

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Characterization of the taxol structure-activity profile for the locus of the A-ring side chain

Abstract

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