Design, synthesis and biological evaluation of some novel sulfonamide derivatives as apoptosis inducers

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorMohamed K.O.
dc.contributor.authorNissan Y.M.
dc.contributor.authorEl-Malah A.A.
dc.contributor.authorAhmed W.A.
dc.contributor.authorIbrahim D.M.
dc.contributor.authorSakr T.M.
dc.contributor.authorMotaleb M.A.
dc.contributor.otherPharmaceutical Organic Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherCairo University
dc.contributor.otherEgypt; Pharmaceutical Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherCairo University
dc.contributor.otherKasr Elini St.
dc.contributor.otherCairo
dc.contributor.other11562
dc.contributor.otherEgypt; Pharmaceutical Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University for Modern Sciences and Arts (MSA)
dc.contributor.otherGiza
dc.contributor.otherEgypt; National Cancer Institute
dc.contributor.otherCancer Biology Department
dc.contributor.otherCairo University
dc.contributor.otherEgypt; Faculty of Science
dc.contributor.otherCairo University
dc.contributor.otherCairo
dc.contributor.otherEgypt; Radioactive Isotopes and Generator Department
dc.contributor.otherHot Labs Center
dc.contributor.otherAtomic Energy Authority
dc.contributor.otherP.O. Box 13759
dc.contributor.otherCairo
dc.contributor.otherEgypt; Labeled Compounds Department
dc.contributor.otherHot Labs Center
dc.contributor.otherAtomic Energy Authority
dc.contributor.otherP.O. Box 13759
dc.contributor.otherCairo
dc.contributor.otherEgypt
dc.date.accessioned2020-01-09T20:41:29Z
dc.date.available2020-01-09T20:41:29Z
dc.date.issued2017
dc.descriptionScopus
dc.descriptionMSA Google Scholar
dc.description.abstractSeveral novel thiazolidinone and fused thiazolidinone derivatives bearing benzenesulfonamide moiety were synthesized and confirmed via spectral and elemental analyses. The newly synthesized compounds were evaluated for their cytotoxic activity on colorectal cancer cell line (Caco-2). All the synthesized compounds showed better activity than the reference standards (Doxorubicin and 5-FU). Investigation of the apoptotic activity of the most active compounds revealed that compounds 3a, 5a, 5c and 6c activate both caspase-3 and Fas-ligand in Caco-2�cell line. Compound 3a was the most active compound with caspase-3 concentration of 0.43�nmol/mL and Fas-ligand concentration of 775.2�pg/mL in treated Caco-2�cells. Compound 3a was radiolabeled with 99mTc and its biodistribution pattern was evaluated in�vivo using normal Swiss Albino mice. 99mTc-compound 3a complex didn't exhibit any accumulation in any body organs except for its accumulation in the colon; target organ; where it showed 8.97���1.35 %ID/g at 15min p. i. that elevated till 16.02���2.43 %ID/g at 120min p. i. � 2017 Elsevier Masson SASen_US
dc.description.urihttps://www.scimagojr.com/journalsearch.php?q=17464&tip=sid&clean=0
dc.identifier.doihttps://doi.org/10.1016/j.ejmech.2017.04.069
dc.identifier.doiPubMed ID 28463785
dc.identifier.issn2235234
dc.identifier.otherhttps://doi.org/10.1016/j.ejmech.2017.04.069
dc.identifier.otherPubMed ID 28463785
dc.identifier.urihttps://t.ly/GgZxb
dc.language.isoEnglishen_US
dc.publisherElsevier Masson SASen_US
dc.relation.ispartofseriesEuropean Journal of Medicinal Chemistry
dc.relation.ispartofseries135
dc.subjectOctober University for Modern Sciences and Arts
dc.subjectجامعة أكتوبر للعلوم الحديثة والآداب
dc.subjectUniversity of Modern Sciences and Arts
dc.subjectMSA University
dc.subjectApoptosisen_US
dc.subjectCaspase-3en_US
dc.subjectFas-liganden_US
dc.subjectRadiolabelingen_US
dc.subjectTechnetium-99�men_US
dc.subjectThiazolidinoneen_US
dc.subject4 [(3 phenylthiazolo[4,5 c]isoxazol 5 yl)amino]benzenesulfonamideen_US
dc.subject4 [(5 benzylidene 4 oxo 4,5 dihydrothiazol 2 yl)amino]benzenesulfonamideen_US
dc.subject4 [(5 oxo 7 phenyl 5,6 dihydrothiazolo[4,5 d]pyrimidin 2yl)amino]benzenesulfonamen_US
dc.subject4 [(7 phenyl 5 thioxo 5,6 dihydrothiazolo[4,5 d]pyrimidin 2 yl)amino]benzenesulfonamideen_US
dc.subject4 [[3 (4 chlorophenyl)thiazolo[4,5 c]isoxazol 5 yl]amino]benzenesulfonamideen_US
dc.subject4 [[3 (4 methoxyphenyl)thiazolo[4,5 c]isoxazol 5 yl]amino]benzenesulfonamideen_US
dc.subject4 [[5 oxo 7 (4 chlorophenyl) 5,6 dihydrothiazolo[4,5 d]pyrimidin 2 yl]amino]benzenesulfonamideen_US
dc.subject4 [[5 oxo 7 (4 methoxyphenyl) 5,6 dihydrothiazolo[4,5-d]pyrimidin 2 yl]amino]benzenesulfonamideen_US
dc.subject4 [[7 (4 chlorophenyl) 5 thioxo 5,6 dihydrothiazolo[4,5 d]pyrimidin 2 yl]amino]benzenesulfonamideen_US
dc.subject4 [[7 (4 methoxyphenyl) 5 thioxo 5,6 dihydrothiazolo[4,5 d]pyrimidin 2 yl]amino]benzenesulfonamideen_US
dc.subjectapoptosis inhibitoren_US
dc.subjectcaspase 3en_US
dc.subjectcytotoxic agenten_US
dc.subjectdoxorubicinen_US
dc.subjectFas liganden_US
dc.subjectfluorouracilen_US
dc.subjectsulfonamideen_US
dc.subjecttechnetium 99men_US
dc.subjectunclassified drugen_US
dc.subjectsulfonamideen_US
dc.subjectalbino mouseen_US
dc.subjectanimal experimenten_US
dc.subjectArticleen_US
dc.subjectCaco-2 cell lineen_US
dc.subjectcontrolled studyen_US
dc.subjectcytotoxicityen_US
dc.subjectdrug designen_US
dc.subjectdrug distributionen_US
dc.subjectdrug screeningen_US
dc.subjectdrug synthesisen_US
dc.subjectin vivo studyen_US
dc.subjectisotope labelingen_US
dc.subjectmouseen_US
dc.subjectnonhumanen_US
dc.subjectstructure activity relationen_US
dc.subjecttarget organen_US
dc.subjectanimalen_US
dc.subjectapoptosisen_US
dc.subjectchemical structureen_US
dc.subjectchemistryen_US
dc.subjectdose responseen_US
dc.subjectdrug effectsen_US
dc.subjecthumanen_US
dc.subjectsynthesisen_US
dc.subjectAnimalsen_US
dc.subjectApoptosisen_US
dc.subjectCaco-2 Cellsen_US
dc.subjectDose-Response Relationship, Drugen_US
dc.subjectDrug Designen_US
dc.subjectHumansen_US
dc.subjectMiceen_US
dc.subjectMolecular Structureen_US
dc.subjectStructure-Activity Relationshipen_US
dc.subjectSulfonamidesen_US
dc.titleDesign, synthesis and biological evaluation of some novel sulfonamide derivatives as apoptosis inducersen_US
dc.typeArticleen_US
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