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Synthesis of pro-apoptotic indapamide derivatives as anticancer agents

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dc.contributor.authorORUN, OYA
dc.contributor.authorsYilmaz, Ozgur; Turan, Suna Ozbas; Akbuga, Julide; Tiber, Pinar Mega; Orun, Oya; Supuran, Claudiu T.; Kucukguzel, S. Guniz
dc.date.accessioned2022-03-14T11:03:37Z
dc.date.available2022-03-14T11:03:37Z
dc.date.issued2015-11-02
dc.description.abstract4-Chloro-3-({[(substitutedamino)carbonothioyl]amino} sulfonyl)-N-(2-methyl-2,3-dihydro-1H-indole-1-yl)benzamide (1-20) and 4-chloro-3-({[3-(substituted)-4-oxo-1,3-thiazolidine-2-ylidene]amino} sulfonyl)-N-(2-methyl-2,3-dihydro-1H-indole-1-yl)benzamide derivatives (21-31) were synthesized from 4-chloro-N-(2-methyl-2,3-dihydroindol-1-yl)-3-sulfamoylbenzamide (indapamide). 4-Chloro-3-({[(4-chlorophenyl)amino)carbonothioyl]amino} sulfonyl)-N-(2-methyl- 2,3-dihydro-1H-indole-1-yl)benzamide 12 demonstrated the highest proapoptotic activity among all synthesized compounds on melanoma cell lines MDA-MB-435 with 3.7% growth inhibition at the concentration of 10 mu M. Compound 12 (SGK 266) was evaluated in vitro using the MTT colorimetric method against melanoma cancer cell line MDA-MB435 growth inhibition for different doses and exhibited anticancer activity with IC50 values of 85-95 mu M against melanoma cancer cell line MDA-MB435. In addition, this compound was investigated as inhibitors of four physiologically relevant human carbonic anhydrase isoforms, hCA I, II, IX and XII. The compund inhibited these enzymes with IC50 values ranging between 0.72 and 1.60 mu M.
dc.identifier.doi10.3109/14756366.2014.1001756
dc.identifier.eissn1475-6374
dc.identifier.issn1475-6366
dc.identifier.pubmed25683085
dc.identifier.urihttps://hdl.handle.net/11424/245810
dc.identifier.wosWOS:000369915500015
dc.language.isoeng
dc.publisherTAYLOR & FRANCIS LTD
dc.relation.ispartofJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectApoptosis
dc.subjectindapamide
dc.subjectsulfonamide
dc.subjectsulphonylthiourea
dc.subject4-thiazolidinone
dc.subjectCARBONIC-ANHYDRASE INHIBITORS
dc.subjectANTI-HCV
dc.subjectCYTOTOXICITY
dc.subjectTHIOUREAS
dc.subject4-THIAZOLIDINONES
dc.subjectIX
dc.titleSynthesis of pro-apoptotic indapamide derivatives as anticancer agents
dc.typearticle
dspace.entity.typePublication
local.avesis.id2d35bf87-a1c2-4afc-b350-6695a8ba17f7
local.import.packageSS16
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atPUBMED
local.journal.numberofpages14
oaire.citation.endPage980
oaire.citation.issue6
oaire.citation.startPage967
oaire.citation.titleJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
oaire.citation.volume30
relation.isAuthorOfPublication21ce2e1a-aeb2-4584-8d4c-1167e0228276
relation.isAuthorOfPublication.latestForDiscovery21ce2e1a-aeb2-4584-8d4c-1167e0228276

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