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dc.creatorKolarević, Ana
dc.creatorIlić, Budimir S.
dc.creatorKocić, Gordana
dc.creatorDžambaski, Zdravko
dc.creatorŠmelcerović, Andrija
dc.creatorBondžić, Bojan
dc.date.accessioned2019-07-02T13:30:31Z
dc.date.available2019-07-02T13:30:31Z
dc.date.issued2018
dc.identifier.issn0730-2312
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2998
dc.description.abstractTwelve new thiazolidinones were synthesized and, together with 41 previously synthesized thiazolidinones, evaluated for inhibitory activity against deoxyribonuclease I (DNase I) in vitro. Ten compounds inhibited commercial bovine pancreatic DNase I with an IC50 below 200 μM and showed to be more potent DNase I inhibitors than crystal violet (IC50 = 365.90 ± 47.33 μM), used as a positive control. Moreover, three compounds were active against DNase I in rat liver homogenate, having an IC50 below 200 μM. (3‐Methyl‐1,4‐dioxothiazolidin‐2‐ylidene)‐N‐(2‐phenylethyl)ethanamide (41) exhibited the most potent DNase I inhibition against both commercial and rat liver DNase I with IC50 values of 115.96 ± 11.70 and 151.36 ± 15.85 μM, respectively. Site Finder and molecular docking defined the thiazolidinones interactions with the most important catalytic residues of DNase I, including the H‐acceptor interaction with residues His 134 and His 252 and/or H‐donor interaction with residues Glu 39 and Asp 168. The three most active compounds against both commercial and rat liver DNase I (31, 38, and 41) exhibited favorable physico‐chemical, pharmacokinetic, and toxicological properties. These observations could be utilized to guide the rational design and optimization of novel thiazolidinone inhibitors. Thiazolidinones as novel DNase I inhibitors could have potential therapeutic applications due to the significant involvement of DNase I in the pathophysiology of many disease conditions.sr
dc.language.isoensr
dc.publisherWileysr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172020/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172044/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/171025/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/31060/RS//sr
dc.rightsrestrictedAccesssr
dc.sourceJournal of Cellular Biochemistrysr
dc.subjectDNase I inhibitionsr
dc.subjectmolecular dockingsr
dc.subjectsynthesissr
dc.subjectthiazolidinonessr
dc.titleSynthesis and DNase I inhibitory properties of some 4‐thiazolidinone derivativessr
dc.typearticlesr
dc.rights.licenseARRsr
dcterms.abstractБонджић, Бојан П.; Коларевић, Aна; Илић, Будимир С.; Коцић, Гордана; Джамбаски, Здравко; Шмелцеровић, Aндрија;
dc.rights.holderWileysr
dc.citation.volume120
dc.citation.issue1
dc.citation.spage264
dc.citation.epage274
dc.citation.rankM22
dc.identifier.doi10.1002/jcb.27339
dc.identifier.scopus2-s2.0-85052832109
dc.identifier.wos000450823500025
dc.type.versionpublishedVersionsr


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