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Ministry of Science and Technology of the Republic of Srpska [19/6-020/961-169/14]

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Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity

Tubić, Biljana K.; Vladimirov, Sandra S.; Marković, Bojan D.; Sabo, Tibor

(Slovensko Kemijsko Drustvo, Ljubljana, 2018)

TY  - JOUR
AU  - Tubić, Biljana K.
AU  - Vladimirov, Sandra S.
AU  - Marković, Bojan D.
AU  - Sabo, Tibor
PY  - 2018
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2113
AB  - 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.
PB  - Slovensko Kemijsko Drustvo, Ljubljana
T2  - Acta Chimica Slovenica
T1  - Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity
VL  - 65
IS  - 1
SP  - 59
EP  - 64
DO  - 10.17344/acsi.2017.3477
ER  - 
@article{
author = "Tubić, Biljana K. and Vladimirov, Sandra S. and Marković, Bojan D. and Sabo, Tibor",
year = "2018",
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.",
publisher = "Slovensko Kemijsko Drustvo, Ljubljana",
journal = "Acta Chimica Slovenica",
title = "Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity",
volume = "65",
number = "1",
pages = "59-64",
doi = "10.17344/acsi.2017.3477"
}
Tubić, B. K., Vladimirov, S. S., Marković, B. D.,& Sabo, T.. (2018). Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity. in Acta Chimica Slovenica
Slovensko Kemijsko Drustvo, Ljubljana., 65(1), 59-64.
https://doi.org/10.17344/acsi.2017.3477
Tubić BK, Vladimirov SS, Marković BD, Sabo T. Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity. in Acta Chimica Slovenica. 2018;65(1):59-64.
doi:10.17344/acsi.2017.3477 .
Tubić, Biljana K., Vladimirov, Sandra S., Marković, Bojan D., Sabo, Tibor, "Prediction of in vivo Bioavailibility by in vitro Characterization of Ethylenediamine Dipropanoic Acid Derivatives with Cytotoxic Activity" in Acta Chimica Slovenica, 65, no. 1 (2018):59-64,
https://doi.org/10.17344/acsi.2017.3477 . .
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