Polyamine conjugates of stigmasterol
Language English Country United States Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
22850319
DOI
10.1016/j.steroids.2012.07.009
PII: S0039-128X(12)00207-3
Knihovny.cz E-resources
- MeSH
- Anti-Bacterial Agents chemical synthesis chemistry pharmacology MeSH
- Chemical Phenomena MeSH
- Carboxylic Acids chemistry MeSH
- Humans MeSH
- Molecular Conformation MeSH
- Models, Molecular MeSH
- Cell Line, Tumor MeSH
- Polyamines chemistry MeSH
- Antineoplastic Agents chemical synthesis chemistry pharmacology MeSH
- Drug Design MeSH
- Staphylococcus aureus drug effects MeSH
- Stigmasterol chemical synthesis chemistry pharmacology MeSH
- Dose-Response Relationship, Drug MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Anti-Bacterial Agents MeSH
- Carboxylic Acids MeSH
- Polyamines MeSH
- Antineoplastic Agents MeSH
- Stigmasterol MeSH
Three new polyamine conjugates with stigmasterol [(3β,22E)-stigmasta-5,22-dien-3-ol] were synthesized and subjected to basic antimicrobial and cytotoxic tests. The conjugate derived from spermine, (3β,22E)-stigmasta-5,22-dien-3-yl 4(12-amino-4,9-diaza-dodecylamino)-4-oxobutanoate (5c), displayed considerable antimicrobial activity on Staphylococcus aureus at low concentration (50 μg mL(-1)). The cytotoxic activity was tested on cells of human T-lymfoblastic leukemia (IC(50)=35.8 ± 10.3 μM (5c) and IC(50)=35.9 ± 5.7 μM (5b)) and normal human fibroblasts (IC(50)=38.0 ± 2.8 μM (5c) and IC(50)=45.5 ± 1.9 μM (5b)). Conjugate 5a displayed no activity in both tests.
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