PRODRUGS FOR NITROREDUCTASE BASED CANCER THERAPY-2: Novel amide/Ntr combinations targeting PC3 cancer cells

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dc.authoridGungor, Tugba/0000-0001-5261-1856
dc.authoridCelik, Ayhan/0000-0003-1355-9252
dc.authoridTASKIN-TOK, Tugba/0000-0002-0064-8400
dc.authoridComert Onder, Ferah/0000-0002-4037-1979
dc.authoridAY, Mehmet/0000-0002-1095-1614
dc.contributor.authorGungor, Tugba
dc.contributor.authorOnder, Ferah Comert
dc.contributor.authorTokay, Esra
dc.contributor.authorGulhan, Unzile Guven
dc.contributor.authorHacioglu, Nelin
dc.contributor.authorTok, Tugba Taskin
dc.contributor.authorCelik, Ayhan
dc.date.accessioned2025-01-27T20:16:40Z
dc.date.available2025-01-27T20:16:40Z
dc.date.issued2019
dc.departmentÇanakkale Onsekiz Mart Üniversitesi
dc.description.abstractThe use of nitroreductases (NTR) that catalyze the reduction of nitro compounds by using NAD(P)H in GDEPT (Gene-directed enzyme prodrug therapy) studies which minimize toxicity at healthy cells and increases concentration of drugs at cancer cells is remarkable. Discovery of new prodrugiNTR combinations is necessary to be an alternative to known prodrug candidates such as CB1954, SN23862, PR 104A. For this aim, nitro containing aromatic amides (A1-A23)(2) were designed, synthesized, performed in silico ADMET and molecular docking techniques in this study. Prodrug candidates were studied on reduction potentials with Ssap-NtrB by HPLC system. Also, cyototoxic properties and prodrug ability of these amides were investigated using different cancer cell lines such as Hep3B and PC3. As a result of theoretical and biological studies, combinations of A5, A6 and A20 with Ssap-NtrB can be suggested as potential prodrugs/enzyme combinations at NTR based cancer therapy compared with CB1954/NfsB. (C) 2019 Elsevier Masson SAS. All rights reserved.
dc.description.sponsorshipScientific and Technological Research Council of Turkey-TUBITAK [110T754, 113Z706]
dc.description.sponsorshipThis study was financially supported by a research grant from Scientific and Technological Research Council of Turkey-TUBITAK (Grant No. 110T754 and 113Z706). Sincere thanks to Gizem TATAR for her supports to help computational part of this study. The numerical calculations reported in this abstract were fully performed at TUBITAK ULAKBIM, High Performance and Grid Computing Center (TRUBA resources).
dc.identifier.doi10.1016/j.ejmech.2019.03.035
dc.identifier.endpage400
dc.identifier.issn0223-5234
dc.identifier.issn1768-3254
dc.identifier.pmid30928710
dc.identifier.scopus2-s2.0-85063547110
dc.identifier.scopusqualityQ1
dc.identifier.startpage383
dc.identifier.urihttps://doi.org/10.1016/j.ejmech.2019.03.035
dc.identifier.urihttps://hdl.handle.net/20.500.12428/21340
dc.identifier.volume171
dc.identifier.wosWOS:000466254500026
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherElsevier France-Editions Scientifiques Medicales Elsevier
dc.relation.ispartofEuropean Journal of Medicinal Chemistry
dc.relation.publicationcategoryinfo:eu-repo/semantics/openAccess
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WoS_20250125
dc.subjectNitro aromatic amides
dc.subjectProdrug
dc.subjectSsap-NtrB
dc.subjectEnzymatic activity
dc.subjectCytotoxicity
dc.subjectMolecular docking
dc.titlePRODRUGS FOR NITROREDUCTASE BASED CANCER THERAPY-2: Novel amide/Ntr combinations targeting PC3 cancer cells
dc.typeArticle

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