Gelişmiş Arama

Basit öğe kaydını göster

dc.contributor.authorVarol, Mehmet
dc.contributor.authorKoparal, Ayşe Tansu
dc.contributor.authorBenkli, Kadriye
dc.contributor.authorBostancıoğlu, Rakibe Beklem
dc.date.accessioned2019-10-20T08:00:46Z
dc.date.available2019-10-20T08:00:46Z
dc.date.issued2018
dc.identifier.issn1567-2018
dc.identifier.issn1875-5704
dc.identifier.urihttps://dx.doi.org/10.2174/1567201815666180727145724
dc.identifier.urihttps://hdl.handle.net/11421/16172
dc.descriptionWOS: 000450647300006en_US
dc.descriptionPubMed ID: 30051790en_US
dc.description.abstractBackground: 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 long-term side effects. Objective: A series of mononuclear gold (III) and platinum (II) complexes based on 4-dihydroxyborylDL-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 TRITC-phalloidin 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.en_US
dc.description.sponsorshipAnadolu University [1101S019 - AUBAP]; TUBITAK [110S077 - SBAG-HD-560]en_US
dc.description.sponsorshipThis study was supported by Anadolu University (Project no: 1101S019 - AUBAP) and TUBITAK (Project no: 110S077 - SBAG-HD-560). Additionally, we would like to thank Anadolu University, Bezmialem Vakif University and Mugla Sitki Kocman University (MSKU), and Assoc. Prof. Resat UNAL from MSKU.en_US
dc.language.isoengen_US
dc.publisherBentham Science Publ LTDen_US
dc.relation.isversionof10.2174/1567201815666180727145724en_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAngiogenesisen_US
dc.subjectDrug Designen_US
dc.subjectNeoplasmen_US
dc.subjectCell Survivalen_US
dc.subjectCisplatinen_US
dc.subjectPhenylalanineen_US
dc.titleAnti-lung Cancer and Anti-angiogenic Activities of New Designed Boronated Phenylalanine Metal Complexesen_US
dc.typearticleen_US
dc.relation.journalCurrent Drug Deliveryen_US
dc.contributor.departmentAnadolu Üniversitesi, Fen Fakültesi, Biyoloji Bölümüen_US
dc.identifier.volume15en_US
dc.identifier.issue10en_US
dc.identifier.startpage1417en_US
dc.identifier.endpage1425en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.contributor.institutionauthorKoparal, Ayşe Tansu
dc.contributor.institutionauthorBenkli, Kadriye


Bu öğenin dosyaları:

DosyalarBoyutBiçimGöster

Bu öğe ile ilişkili dosya yok.

Bu öğe aşağıdaki koleksiyon(lar)da görünmektedir.

Basit öğe kaydını göster