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Synthesis, Characterisation and Biological Evaluation of Copper and Silver Complexes based on Acetylsalicylic Acid
Author(s) -
Rubner Gerhard,
Bensdorf Kerstin,
Wellner Anja,
Bergemann Silke,
Gust Ronald
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000382
Subject(s) - copper , chemistry , combinatorial chemistry , biological activity , biochemistry , organic chemistry , in vitro
Metalcarbonyl complexes with ligands derived from acetylsalicylic acid demonstrated high cytotoxic potential against various tumor cell lines and strong inhibition of the cyclooxygenase enzymes COX‐1 and 2. In this study we tried to achieve comparable effects with [alkyne]silver or copper trifluoromethanesulfonate complexes which are more hydrophilic then the uncharged metalcarbonyl derivatives. All compounds were evaluated for growth inhibition against breast (MCF‐7, MDA‐MB 231) and colon cancer (HT‐29) cell lines and for COX‐1 and COX‐2 inhibitory effects at isolated isoenzymes. Pure ligands showed neither cytotoxic nor COX‐inhibitory effects. While the silver complexes of (but‐2‐ynyl)‐2‐acetoxybenzoate ( But‐ASS‐Ag ) and (but‐2‐yne‐1,4‐diyl)‐bis(2‐acetoxybenzoate) ( Di‐ASS‐But‐Ag ) were strong cytostatics, only the copper complex Di‐ASS‐But‐Cu was active. At the COX enzymes the complexes were more effective than their ligands and aspirin.