Synthesis, anticancer activity and ADMET studies of N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido] benzenesulfonamide derivatives

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dc.authoridTok, Fatih/0000-0002-4569-008X
dc.authoridSalva, Emine/0000-0002-1159-5850
dc.authoridTASKIN TOK, Tugba/0000-0002-0064-8400
dc.authoridŞALVA, EMINE/0000-0002-1159-5850
dc.authoridKaymakçıoğlu, Bedia/0000-0003-0817-8236
dc.authoridTatar Yilmaz, Gizem/0000-0001-6642-6870
dc.authorwosidturk, sevda/AAR-2168-2020
dc.authorwosidTok, Fatih/AAA-3038-2019
dc.authorwosidSalva, Emine/ABI-2766-2020
dc.authorwosidKocyigit-Kaymakcioglu, Bedia/JOZ-6092-2023
dc.authorwosidTASKIN TOK, Tugba/A-8885-2016
dc.authorwosidTatar Yılmaz, Gizem/I-6440-2018
dc.authorwosidKarakuş, Sevgi/AAI-4259-2020
dc.contributor.authorKarakus, S.
dc.contributor.authorTok, F.
dc.contributor.authorTuerk, S.
dc.contributor.authorSalva, E.
dc.contributor.authorTatar, G.
dc.contributor.authorTaskin-Tok, T.
dc.contributor.authorKocyigit-Kaymakcioglu, B.
dc.date.accessioned2024-08-04T20:44:25Z
dc.date.available2024-08-04T20:44:25Z
dc.date.issued2018
dc.departmentİnönü Üniversitesien_US
dc.description.abstractA series of novel 4-[(3-substituted)ureido]-N-(5-methyl-1,3,4-thiadiazol-2-yl) benzenesulfonamides and 4-[(3-substituted)thioureido]-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamides were prepared from 4-amino-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide (sulfamethizole). The structures of the synthesized compounds were determined by IR, H-1-NMR, MS and elemental analysis. The anticancer activity of these compounds was evaluated against human colorectal carcinoma (HCT116) and human cervix carcinoma (HeLa) cell lines. Compound 4 (4-{[(2,4-dichlorophenyl)carbamoyl]amino}-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide) showed marked anticancer activity, being the most active compounds in this series with the IC50 value of 13.92 +/- 0.22 mu M and 37.91 +/- 0.10 mu M against HeLa and HCT116, respectively. In silico, ADMET was used to examine their pharmacokinetic properties. ADMET (absorption, distribution, metabolism, excretion, and toxicity) studies were applied to develop new anticancer compound(s) with high selectivity. [GRAPHICS] .en_US
dc.identifier.doi10.1080/10426507.2018.1452924
dc.identifier.endpage534en_US
dc.identifier.issn1042-6507
dc.identifier.issn1563-5325
dc.identifier.issue8en_US
dc.identifier.scopus2-s2.0-85045197368en_US
dc.identifier.scopusqualityQ4en_US
dc.identifier.startpage528en_US
dc.identifier.urihttps://doi.org/10.1080/10426507.2018.1452924
dc.identifier.urihttps://hdl.handle.net/11616/98236
dc.identifier.volume193en_US
dc.identifier.wosWOS:000438408900009en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofPhosphorus Sulfur and Silicon and The Related Elementsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectUreaen_US
dc.subjectthioureaen_US
dc.subjectanticancer activityen_US
dc.subjectin silico ADMETen_US
dc.titleSynthesis, anticancer activity and ADMET studies of N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido] benzenesulfonamide derivativesen_US
dc.typeArticleen_US

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