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Further exploration of DVD-445 as a lead thioredoxin reductase (TrxR) inhibitor for cancer therapy: Optimization of potency and evaluation of anticancer potential.
| dc.creator | Jovanović, Mirna | |
| dc.creator | Zhukovsky, Daniil | |
| dc.creator | Podolski-Renić, Ana | |
| dc.creator | Žalubovskis, Raivis | |
| dc.creator | Dar'in, Dmitry | |
| dc.creator | Sharoyko, Vladimir | |
| dc.creator | Tennikova, Tatiana | |
| dc.creator | Pešić, Milica | |
| dc.creator | Krasavin, Mikhail | |
| dc.date.accessioned | 2020-02-27T11:59:55Z | |
| dc.date.available | 2900-01-01 | |
| dc.date.issued | 2020 | |
| dc.identifier.issn | 0223-5234 | |
| dc.identifier.uri | https://radar.ibiss.bg.ac.rs/handle/123456789/3614 | |
| dc.description.abstract | A series of analogs of the earlier reported lead compound DVD-445 (thioredoxin reductase inhibitor with anticancer activity) has been synthesized via a modified Ugi reaction and investigated. Seven most potent compounds (with IC50 below 5.00 μM against recombinant rTrxR1 enzyme) were examined for their effect on cell growth and viability, oxidative stress induction and P-glycoprotein (P-gp) inhibition in human glioblastoma cells cell line U87 and its corresponding multidrug resistant (MDR) cell line U87-TxR. Several of these frontrunner compounds were shown to be superior over DVD-445. Besides providing promising candidates for anticancer therapy, our study further validates the small electrophilic Ugi Michael acceptor (UMA) chemotype as efficacious inhibitor of thioredoxin reductase. | en |
| dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41031/RS// | |
| dc.relation | ERA.Net RUS plus joint program grant RUS_ST2017-309 | |
| dc.relation | Russian Foundation for Basic Research (project grant 18–515-76001) | |
| dc.relation | State Education Development Agency of Republic of Latvia (“THIOREDIN”) | |
| dc.rights | restrictedAccess | |
| dc.source | European Journal of Medicinal Chemistry | |
| dc.subject | Cancer cell defense mechanism | |
| dc.subject | Covalent inhibitor | |
| dc.subject | Michael acceptors | |
| dc.subject | Oxidative stress | |
| dc.subject | P-gp inhibition | |
| dc.subject | Thioredoxin reductase | |
| dc.subject | Ugi four-component reaction | |
| dc.title | Further exploration of DVD-445 as a lead thioredoxin reductase (TrxR) inhibitor for cancer therapy: Optimization of potency and evaluation of anticancer potential. | en |
| dc.type | article | en |
| dc.rights.license | ARR | |
| dcterms.abstract | Подолски-Ренић, Aна; Красавин, Микхаил; Јовановић, Мирна; Зхуковскy, Даниил; Жалубовскис, Раивис; Дар'ин, Дмитрy; Схароyко, Владимир; Тенникова, Татиана; Пешић, Милица; | |
| dc.rights.holder | © 2020 Elsevier Masson SAS. | |
| dc.citation.volume | 191 | |
| dc.identifier.doi | 10.1016/j.ejmech.2020.112119 | |
| dc.identifier.pmid | 32087464 | |
| dc.identifier.scopus | 2-s2.0-85079530936 | |
| dc.identifier.wos | 000523562700011 | |
| dc.citation.apa | Jovanović, M., Zhukovsky, D., Podolski-Renić, A., Žalubovskis, R., Dar’in, D., Sharoyko, V., et al. (2020). Further exploration of DVD-445 as a lead thioredoxin reductase (TrxR) inhibitor for cancer therapy: Optimization of potency and evaluation of anticancer potential. European Journal of Medicinal Chemistry, 191, 112119. | |
| dc.citation.vancouver | Jovanović M, Zhukovsky D, Podolski-Renić A, Žalubovskis R, Dar’in D, Sharoyko V, Tennikova T, Pešić M, Krasavin M. Further exploration of DVD-445 as a lead thioredoxin reductase (TrxR) inhibitor for cancer therapy: Optimization of potency and evaluation of anticancer potential. Eur J Med Chem. 2020;191:112119. | |
| dc.citation.spage | 112119 | |
| dc.type.version | publishedVersion | |
| dc.citation.rank | aM21 |
