Back to Search
Start Over
Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2016 Sep 15; Vol. 24 (18), pp. 4120-4128. Date of Electronic Publication: 2016 Jun 27. - Publication Year :
- 2016
-
Abstract
- Oblongifolin C, one of the polyprenylated benzoylphloroglucinol natural products (PPAPs) isolated from the fruits of Garcinia yunnanensis Hu, was recently discovered to be a potent anti-tumor agent. A collection of 12 derivatives with modifications on the benzophenone moieties were synthesized and tested for c-Met kinase inhibition and cytotoxicity against the HepG2, Miapaca-2, HCC827, Hela, A549, AGS, and HT-29 cell lines in vitro. An oxidized derivative, 10, was found to possess strong inhibition and anti-migration properties in the HCC827 cell line and serves as a potential lead compound for the development of new anticancer drugs. In addition, structure-activity relationships (SAR) were also evaluated to provide key information for future anticancer drug development.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antineoplastic Agents, Phytogenic chemical synthesis
Benzophenones chemical synthesis
Benzophenones chemistry
Benzophenones pharmacology
Cell Line, Tumor
Drug Screening Assays, Antitumor
Garcinia chemistry
HT29 Cells
HeLa Cells
Humans
Neoplasms drug therapy
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors pharmacology
Proto-Oncogene Proteins c-met metabolism
Structure-Activity Relationship
Terpenes chemical synthesis
Antineoplastic Agents, Phytogenic chemistry
Antineoplastic Agents, Phytogenic pharmacology
Proto-Oncogene Proteins c-met antagonists & inhibitors
Terpenes chemistry
Terpenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 24
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27396929
- Full Text :
- https://doi.org/10.1016/j.bmc.2016.06.054