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Synthesis of novel α-santonin derivatives as potential cytotoxic agents
- Source :
- LOCUS Repositório Institucional da UFV, Universidade Federal de Viçosa (UFV), instacron:UFV
- Publication Year :
- 2010
- Publisher :
- Elsevier BV, 2010.
-
Abstract
- Ten novel a -santonin derivatives have been synthesized as cytotoxic agents. The in vitro antitumor activity of these compounds has been evaluated against cancer cells lines. Structure-activity relationships indicate that a -methylene- g -lactone and endoperoxide functionalities play important roles in conferring cytotoxicity. The compounds 2e4, possessing the a -methylene- g -lactone group showed IC 50 values between 5.70 and 16.40 m M. Mixture of isomers 5 and 6, with the a -methylene- g -lactone and endoperoxide functionalities, displayed the greatest activity, with IC 50 values between 1.45 and 4.35 m M. The biological assays conducted with normal cells revealed that the compounds 2, 5 and 6 are selective against cancer cells lines tested. Bioactive lactones described herein and in our previous report did not cause disruption of the cell membrane in mouse erythrocytes.
- Subjects :
- Stereochemistry
Cytotoxicity
Antineoplastic Agents
HL-60 Cells
Peripheral blood mononuclear cell
Chemical synthesis
Cell membrane
Structure-Activity Relationship
Cell Line, Tumor
Drug Discovery
medicine
Humans
Parishin A synthesis
Endoperoxide bridge
Cell Proliferation
Pharmacology
chemistry.chemical_classification
Molecular Structure
Organic Chemistry
Stereoisomerism
General Medicine
In vitro
medicine.anatomical_structure
chemistry
Biochemistry
Cell culture
Cancer cell
α-methylene-γ-lactone
Drug Screening Assays, Antitumor
Santonin
Sesquiterpene lactones
Lactone
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 45
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....d110edfd50959a789957cf996b98421d