Background: Drug design and discovery studies still remain of great importance in the
search for more convenient chemotherapeutic to avoid the drug resistance, systemic toxicity or the longterm
Objective: A series of mononuclear gold (III) and platinum (II) complexes based on 4-dihydroxyboryl-
DL-phenylalanine (BPA) was designed and synthesized, for the first time, by using 2, 2’-dipyridyl (L1)
and 4, 4’-diaminobibenzyl (L2) ligands. Characterization of the synthesized complexes was achieved by
using 1H-NMR, IR, MS and elemental analyses.
Method: MTT cell viability, endothelial tube formation, cancer cell colony formation and TRITCphalloidin
cytoskeleton staining assays were performed on human umbilical vein endothelial (HUVEC)
and human lung adenocarcinoma (A549) cells to establish the anticancer and anti-angiogenic activities
of the complexes. It was determined that the organometallic complexes that include 2, 2’-dipyridyl
ligand have higher antiproliferative activity than L2-based complexes in the micromolar range. Colony
formation experiments showed that the anchorage-independent growth ability of A549s was significantly
affected by the complexes in a concentration-dependent manner though L1-based complexes
were more effective than L2-based ones.
Results: It was also clearly observed that the complexes have significant anti-angiogenic and cytoskeleton
alterative activities. Consequently, the phenylalanine-based organometallic complexes seem to have
anti-lung cancer and anti-angiogenic activities depending on the ligand type and a great potential in
oncology drug development because phenylalanine amino acid has an ability to cross the cell membrane
by using L-amino acid transport system.
Conclusion: Design, synthesis and activity studies with amino acid analogs should be therefore increased
to discover more efficient drugs to cure cancer diseases.