Synthesis and biological studies of some gold(I) complexes containing functionalised alkynes.
The propargyl ethers 7-chloro-(4-propargyloxy)quinoline, 1-propargyloxynaphthalene and 2-propargyloxybenzophenone react with [AuCl(PPh(3))] in the presence of KOH to give the gold(I) alkynyl complexes [Au(C[triple bond]COCH(2)Ar)(PPh(3))] in good yields. The compounds were fully characterised by spectroscopic methods and were subsequently examined for their biological activity against four tumour cell lines as well as their activity against Plasmodium falciparum, the parasite responsible for malaria. The compounds show antiproliferative effects in human cancer cells with IC(50) values ranging from 0.4-12 microM.
Schuh
Esther
E
Fachbereich C, Anorganische Chemie Bergische Universität Wuppertal, Gaussstr. 20, D-42929, Wuppertal, Germany.
Valiahdi
Seied M
SM
Jakupec
Michael A
MA
Keppler
Bernhard K
BK
Chiba
Peter
P
Mohr
Fabian
F
D000480:Alkynes / Q000737:chemistry*; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001577:Benzophenones / Q000737:chemistry; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D004354:Drug Screening Assays, Antitumor; D006046:Gold / Q000737:chemistry*; D006801:Humans; D009281:Naphthalenes / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects; D011804:Quinolines / Q000737:chemistry
D000480:Alkynes; D000962:Antimalarials; D000970:Antineoplastic Agents; D001577:Benzophenones; D056831:Coordination Complexes; D009281:Naphthalenes; D011804:Quinolines; C031721:naphthalene; C047723:benzophenone; D006046:Gold; C037219:quinoline