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Synthesis of novel strobilurin-pyrimidine derivatives and their antiproliferative activity against human cancer cell lines.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Jun 15; Vol. 23 (12), pp. 3505-10. Date of Electronic Publication: 2013 Apr 26. - Publication Year :
- 2013
-
Abstract
- A series of new strobilurin-pyrimidine analogs were designed and synthesized based on the structures of our previously discovered antiproliferative compounds I and II. Biological evaluation with two human cancer cell lines (A549 and HL60) showed that most of these compounds possessed moderate to potent antiproliferative activity. Two potent candidates (8f, IC50=2.2 nM and 11d, IC50=3.4 nM) were identified with nanomolar activity against leukemia cancer cell line HL60 for further development. This activity represents a 1000- to 2500-fold improvement compared to the parent compounds I and II and is 20- to 30-fold better than the chemotherapy drug, doxorubicin. The present work provides strong incentive for further development of these strobilurin-pyrimidine analogs as potential antitumor agents for the treatment of leukemia.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Cell Line, Tumor
Cell Proliferation drug effects
Drug Screening Assays, Antitumor
Fatty Acids, Unsaturated chemistry
HL-60 Cells
Humans
Leukemia pathology
Lung Neoplasms pathology
Methacrylates chemical synthesis
Methacrylates chemistry
Methacrylates pharmacology
Pyrimidines chemistry
Structure-Activity Relationship
Fatty Acids, Unsaturated chemical synthesis
Fatty Acids, Unsaturated pharmacology
Leukemia drug therapy
Lung Neoplasms drug therapy
Pyrimidines chemical synthesis
Pyrimidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Report
- Accession number :
- 23664877
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.04.045