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Antiproliferative Activity of Polyether Antibiotic – Cinchona Alkaloid Conjugates Obtained via Click Chemistry
Author(s) -
Skiera Iwona,
Antoszczak Michał,
Trynda Justyna,
Wietrzyk Joanna,
Boratyński Przemysław,
Kacprzak Karol,
Huczyński Adam
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12523
Subject(s) - salinomycin , chemistry , alkaloid , cinchona , click chemistry , conjugate , propargyl , cycloaddition , indolizidine , propargyl alcohol , stereochemistry , brucine , in vitro , combinatorial chemistry , organic chemistry , enantioselective synthesis , antibiotics , biochemistry , catalysis , mathematical analysis , mathematics , strychnine
A series of eight new conjugates of salinomycin or monensin and Cinchona alkaloids were obtained by the Cu(I)‐catalysed 1,3‐dipolar Huisgen cycloaddition (click chemistry) of respective N ‐propargyl amides of salinomycin or monensin with four different Cinchona alkaloid derived azides. In vitro antiproliferative activity of these conjugates evaluated against three cancer cell lines (LoVo, LoVo/ DX , HepG2) showed that four of the compounds exhibited high antiproliferative activity ( IC 50 below 3.00 μ m ) and appeared to be less toxic and more selective against normal cells than two standard anticancer drugs.