Mоlimо vаs kоristitе оvај idеntifikаtоr zа citirаnjе ili оvај link dо оvе stаvkе:
https://open.uns.ac.rs/handle/123456789/3272
Nаziv: | Evaluation of in silico pharmacokinetic properties and in vitro cytotoxic activity of selected newly synthesized N-succinimide derivatives | Аutоri: | Milošević, Nataša Kojić, Vesna Ćurčić, Jelena Jakimov D. Milić, Neda Banjac N. Uscumlic G. Kaliszan R. |
Dаtum izdаvаnjа: | 15-апр-2017 | Čаsоpis: | Journal of Pharmaceutical and Biomedical Analysis | Sažetak: | © 2017 Elsevier B.V. Design of a new drug entity is usually preceded by analysis of quantitative structure activity (properties) relationships, QSA(P)R. Six newly synthesized succinimide derivatives have been determined for (i) in silico physico-chemical descriptors, pharmacokinetic and toxicity predictors, (ii) in vitro biological activity on four different carcinoma cell lines and on normal fetal lung cells and (iii) lipophilicity on liquid chromatography. All compounds observed were predicted for good permeability and solubility, good oral absorption rate and moderate volume of distribution as well as for modest blood brain permeation, followed by acceptable observed toxicity. In silico determined lipophilicity, permeability through jejunum and aqueous solubility were correlated with experimentally obtained lipophilic constants (by use of high pressure liquid chromatography) and linear correlations were obtained. Absorption rate and volume of distribution were predicted by chromatographic lipophilicity measurements while permeation through blood bran barrier was predicted dominantly by molecular size defined with molecular weight. Five compounds have demonstrated antiproliferative activity toward cervix carcinoma HeLa cell lines; three were cytotoxic against breast carcinoma MCF-7 cells, while one inhibited proliferation of colon carcinoma HT-29 cell lines. Only one compound was cytotoxic toward normal cell lines, while other compounds were proven as safe. Antiproliferative potential against HeLa cells was described as exponential function of lipophilicity. Based on obtained results, lead compounds were selected. | URI: | https://open.uns.ac.rs/handle/123456789/3272 | ISSN: | 7317085 | DOI: | 10.1016/j.jpba.2017.01.042 |
Nаlаzi sе u kоlеkciјаmа: | FTN Publikacije/Publications |
Prikаzаti cеlоkupаn zаpis stаvki
SCOPUSTM
Nаvоđеnjа
20
prоvеrеnо 10.05.2024.
Prеglеd/i stаnicа
28
Prоtеklа nеdеljа
12
12
Prоtеkli mеsеc
1
1
prоvеrеnо 10.05.2024.
Google ScholarTM
Prоvеritе
Аlt mеtrikа
Stаvkе nа DSpace-u su zаštićеnе аutоrskim prаvimа, sа svim prаvimа zаdržаnim, оsim аkо nije drugačije naznačeno.