Back to Search
Start Over
One-pot synthesis and cytotoxicity studies of new Mannich base derivatives of polyether antibiotic--lasalocid acid.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Sep 15; Vol. 23 (18), pp. 5053-6. Date of Electronic Publication: 2013 Jul 26. - Publication Year :
- 2013
-
Abstract
- Seven Mannich base derivatives of polyether antibiotic Lasalocid acid (2a-2g) were synthesized and screened for their antiproliferative activity against various human cancer cell lines. A novel chemoselective one-pot synthesis of these Mannich bases was developed. Compounds 2a-2c and 2g with sterically smaller dialkylamine substituent, displayed potent antiproliferative activity (IC50: 3.2-7.3 μM), and demonstrated higher than twofold selectivity for specific type of cancer. The nature of Mannich base substituent on C-2 atom at the aromatic ring may be critical in the search for selectivity towards a particular cancer cell.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anti-Bacterial Agents chemistry
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
HT29 Cells
Humans
Lasalocid chemical synthesis
Lasalocid chemistry
MCF-7 Cells
Molecular Conformation
Structure-Activity Relationship
Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents pharmacology
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Lasalocid analogs & derivatives
Lasalocid pharmacology
Mannich Bases chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 23932361
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.07.040