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Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity
dc.creator | Tubić, Biljana | |
dc.creator | Vladimirov, Sandra | |
dc.creator | Marković, Bojan | |
dc.creator | Sabo, Tibor | |
dc.date.accessioned | 2019-09-02T12:06:20Z | |
dc.date.available | 2019-09-02T12:06:20Z | |
dc.date.issued | 2018 | |
dc.identifier.issn | 1318-0207 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/3156 | |
dc.description.abstract | O,O'-diethyl-(S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoate (DE-EDCP) is novel substance with cytotoxic activity in human leukemic cells. The aim of this study has been to predict in vivo bioavailability of the DE-EDCP and its potential metabolite (S, S)-ethylenediamine-N, N'-di-2-(3-cyclohexyl) propanoic acid (EDCP) by in vitro characterization which includes determination of lipophilicity and passive membrane permeability. There has also been evaluated inter-laboratory reproducibility of the bio-analytical method which was previously developed and validated for non-clinical study of the DE-EDCP and EDCP. Distribution coefficient n-octanol/water was 1.68 and 0.03, and apparent permeability coefficient was 4 x 10(-4) cm/s and 20 x 10(-4) cm/s, for the DE-EDCP and EDCP, respectively. Observed results have shown that the DE-EDCP is more lipophilic with better membrane retention, but the EDCP has better pass through the membrane. Also, there has been demonstrated a reproducibility and robustness of the proposed bio-analytical method. | en |
dc.publisher | Slovensko Kemijsko Drustvo, Ljubljana | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS// | |
dc.rights | openAccess | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | Acta Chimica Slovenica | |
dc.subject | Transfer of the UHPLC-MS/MS | en |
dc.subject | cross validation | en |
dc.subject | (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl) propanoic acid esters | en |
dc.subject | membrane permeability | en |
dc.subject | lipophilicity | en |
dc.title | Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity | en |
dc.type | article | |
dc.rights.license | BY | |
dcterms.abstract | Тубић, Биљана; Марковић, Бојан; Сабо, Тибор; Владимиров, Сандра; | |
dc.citation.volume | 65 | |
dc.citation.issue | 1 | |
dc.citation.spage | 59 | |
dc.citation.epage | 64 | |
dc.citation.other | 65(1): 59-64 | |
dc.citation.rank | M23 | |
dc.identifier.wos | 000428179900006 | |
dc.identifier.doi | 10.17344/acsi.2017.3477 | |
dc.identifier.pmid | 29562114 | |
dc.identifier.scopus | 2-s2.0-85044361213 | |
dc.identifier.fulltext | https://farfar.pharmacy.bg.ac.rs//bitstream/id/1739/3154.pdf | |
dc.type.version | publishedVersion |