Design and semisynthesis of novel fredericamycin A derivatives with an improved antitumor profile

Starting from natural Fredericamycin A, a series of semisynthetic derivatives was prepared exhibiting increased potency and selectivity in vitro in a human tumor cell line panel. We report the design, semisynthesis, and biological activity of a series of fredericamycin ( 1) derivatives. Within this...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (12), p.3292-3297
Main Authors: Abel, Ulrich, Simon, Werner, Eckard, Peter, Hansske, Friedrich G.
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antineoplastic Agents - toxicity
Antitumor
Biological and medical sciences
Cell Line
Cell Survival - drug effects
Drug Design
Fredericamycin
General aspects
Humans
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Isoquinolines - pharmacology
Isoquinolines - toxicity
Medical sciences
Mice
Mice, Nude
Molecular Structure
Natural product
Pharmacology. Drug treatments
Semisynthesis
Spiro Compounds - chemical synthesis
Spiro Compounds - chemistry
Spiro Compounds - pharmacology
Spiro Compounds - toxicity
Spiro quinone
Structure-Activity Relationship
Xenograft Model Antitumor Assays
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Summary:Starting from natural Fredericamycin A, a series of semisynthetic derivatives was prepared exhibiting increased potency and selectivity in vitro in a human tumor cell line panel. We report the design, semisynthesis, and biological activity of a series of fredericamycin ( 1) derivatives. Within this series compound 1e combines low nanomolar cytotoxic potency in vitro, increased tumor cell line selectivity, and in vivo activity in a human xenograft model.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.03.029