Cytotoxic Simplified Tubulysin Analogues

An efficient route for the synthesis of the tubulysin family of antimitotic peptides was developed. Simplified tubulysin analogues were synthesized to define the minimum pharmacophore required for cytotoxicity. Simplified tubulysin analogues retain significant cytotoxicity and reveal important preli...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2008-03, Vol.51 (6), p.1530-1533
Main Authors: Raghavan, Bhooma, Balasubramanian, Ranganathan, Steele, Jaeson C, Sackett, Dan L, Fecik, Robert A
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor
Cell Proliferation - drug effects
Dose-Response Relationship, Drug
Drug Design
Drug Screening Assays, Antitumor
General aspects
Humans
Medical sciences
Molecular Conformation
Oligopeptides - chemical synthesis
Oligopeptides - chemistry
Oligopeptides - pharmacology
Pharmacology. Drug treatments
Structure-Activity Relationship
Time Factors
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Summary:An efficient route for the synthesis of the tubulysin family of antimitotic peptides was developed. Simplified tubulysin analogues were synthesized to define the minimum pharmacophore required for cytotoxicity. Simplified tubulysin analogues retain significant cytotoxicity and reveal important preliminary structure–activity relationships.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm701321p