Synthesis and cytotoxicity of podophyllotoxin analogues modified in the A ring

Several podophyllotoxin derivatives lacking the methylenedioxy group or with different functionalization of the A-ring of the cyclolignan skeleton have been prepared and evaluated for their cytotoxic activities on four neoplastic cell lines (P-388, A-549, HT-29 and MEL-28). Most of them maintained t...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2003, Vol.38 (1), p.65-74
Main Authors: Castro, Angeles, del Corral, José M.Miguel, Gordaliza, Marina, Grande, Concepción, Gómez-Zurita, Antonia, Garcı́a-Grávalos, Dolores, San Feliciano, Arturo
Format: Article
Language:English
Subjects:
A-ring modifications
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor - drug effects
Cyclolignans
Cytotoxicity
Dioxanes - chemical synthesis
Dioxanes - pharmacology
Dioxoles - chemical synthesis
Dioxoles - chemistry
Dioxoles - pharmacology
Drug Screening Assays, Antitumor
General aspects
Humans
Lignans - chemical synthesis
Lignans - pharmacology
Magnetic Resonance Spectroscopy
Medical sciences
Mice
Models, Chemical
Molecular Structure
Pharmacology. Drug treatments
Podophyllotoxin
Podophyllotoxin - analogs & derivatives
Podophyllotoxin - pharmacology
Structure-Activity Relationship
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Description
Summary:Several podophyllotoxin derivatives lacking the methylenedioxy group or with different functionalization of the A-ring of the cyclolignan skeleton have been prepared and evaluated for their cytotoxic activities on four neoplastic cell lines (P-388, A-549, HT-29 and MEL-28). Most of them maintained their cytotoxicity at the μM level.
ISSN:0223-5234
1768-3254
DOI:10.1016/S0223-5234(02)00007-7