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Design and synthesis of novel organometallic complexes using boronated phenylalanine derivatives as potential anticancer agents

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dc.contributor.authorVarol, Mehmet
dc.contributor.authorBenkli, KADRİYE
dc.contributor.authorKoparal, Ayse T.
dc.contributor.authorBostancioglu, Rakibe B.
dc.contributor.institutionauthorBENKLİ, KADRIYE
dc.date.accessioned2019-10-05T12:47:52Z
dc.date.available2019-10-05T12:47:52Z
dc.date.issued2019-07-04
dc.description.abstractDrug design and discovery studies are important because of the prevalence of diseases without available medical cures. New anticancer agents are particularly urgent because of the high mortality rate associated with cancer. A series of mononuclear gold (III) and platinum (II) complexes based on boronated phenylalanine (BPA) were designed and synthesized using 4,4--dimethyl-2,2--dipyridyl (L1) or 1,10-phenanthroline-5,6-dion (L2) ligands to obtain promising anticancer drug candidates. Proton nuclear magnetic resonance, infrared, mass spectrometry, and elemental analyses were utilized for chemical characterizations. Cell viability, cancer cell colony formation, endothelial tube formation, and cytoskeleton staining assays were performed using A549 lung adenocarcinoma and human umbilical vein endothelial cells (HUVECs) to investigate preliminary pharmacological activities. L1-based platinum (II) complex (BPA-L1-Pt) was the most promising complex, and has similar activity with the approved chemotherapy drug cis-platinum. Half maximal inhibitory concentration values for BPA-L1-Pt were 9.15 mu M on A549s and 16.61 mu M on HUVECs; the values for cis-platinum were 5.24 mu M on A549s and 23.14 mu M on HUVECs. Consequently, further synthesis studies should be performed to boost the cancer cell selectivity feature of BPA by varying metal and ligand types.
dc.description.sponsorshipTürkiye Bilimsel Ve Teknolojik Araştırma Kurumu ( Tübitak )
dc.identifier10.5114/wo.2014.40556
dc.identifier.citationVarol M., Benkli K., Koparal A. T. , Bostancioglu R. B. , -Design and synthesis of novel organometallic complexes using boronated phenylalanine derivatives as potential anticancer agents-, DRUG AND CHEMICAL TOXICOLOGY, cilt.42, ss.436-443, 2019
dc.identifier.doi10.1080/01480545.2018.1504057
dc.identifier.pubmed30208738
dc.identifier.scopus85053468112
dc.identifier.urihttps://hdl.handle.net/20.500.12645/599
dc.identifier.wosWOS:000466854400012
dc.language.isoen
dc.titleDesign and synthesis of novel organometallic complexes using boronated phenylalanine derivatives as potential anticancer agents
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameWspolczesna Onkologia
local.avesis.id0bf6c0e9-31f3-4c44-9115-e66bca77bf37
local.avesis.response469
local.org.facultyTıp Fakültesi
local.publication.goal03 - Sağlık ve Kaliteli Yaşam
local.publication.isinternational1
relation.isAuthorOfPublication7c79666b-9d7a-4020-a3f2-da0a94989b66
relation.isAuthorOfPublication.latestForDiscovery7c79666b-9d7a-4020-a3f2-da0a94989b66
relation.isGoalOfPublication9c198c48-b603-4e2f-8366-04edcfc1224c
relation.isGoalOfPublication.latestForDiscovery9c198c48-b603-4e2f-8366-04edcfc1224c
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