1,2-Dithiolan-3-ones and derivatives structurally related to leinamycin. Synthesis and biological evaluation

Leinamycin, an antitumor antibiotic isolated from Streptomyces sp., shows a 1,2-dithiolan-3-one 1-oxide heterocycle that appears to be involved in the biological activity. Several derivatives related to 1,2-dithiolan-3-one 1-oxide have been prepared and their activity as antineoplastic agents have b...

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Bibliographic Details
Published in:Farmaco (Società chimica italiana : 1989) 2003-09, Vol.58 (9), p.995-998
Main Authors: Salvetti, Raul, Martinetti, Giovanni, Ubiali, Daniela, Pregnolato, Massimo, Pagani, Giuseppe
Format: Article
Language:English
Subjects:
1,2-Dithiolan-3-ones-1-oxide
Antineoplastic activity
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Line, Tumor
Drug Design
Drug Screening Assays, Antitumor
Heterocyclic Compounds, 2-Ring - chemical synthesis
Heterocyclic Compounds, 2-Ring - chemistry
Heterocyclic Compounds, 2-Ring - pharmacology
Humans
Lactams
Leinamycin
Macrolides - chemistry
Sulfhydryl Compounds - chemistry
Sulfhydryl Compounds - pharmacology
Thiazoles - chemistry
Thiones - chemistry
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Summary:Leinamycin, an antitumor antibiotic isolated from Streptomyces sp., shows a 1,2-dithiolan-3-one 1-oxide heterocycle that appears to be involved in the biological activity. Several derivatives related to 1,2-dithiolan-3-one 1-oxide have been prepared and their activity as antineoplastic agents have been investigated. The synthesized compounds did not display a significative antitumor or cytotoxic activity in vitro.
ISSN:0014-827X
1879-0569
DOI:10.1016/S0014-827X(03)00134-4