One-pot synthesis and cytotoxicity studies of new Mannich base derivatives of polyether antibiotic--lasalocid acid.
Basic Information
ID: ALA2417465
Journal: Bioorg Med Chem Lett
Title: One-pot synthesis and cytotoxicity studies of new Mannich base derivatives of polyether antibiotic--lasalocid acid.
Authors: Huczyński A, Rutkowski J, Borowicz I, Wietrzyk J, Maj E, Brzezinski B.
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.
CiteXplore: 23932361
DOI: 10.1016/j.bmcl.2013.07.040
Patent ID: ┄