Publication:
Design, synthesis and biological evaluation of novel triazolothiadiazoles derived from NSAIDs as anticancer agents

dc.contributor.coauthorAytaç, Peri
dc.contributor.coauthorAtalay, Rengül Çetin
dc.contributor.coauthorTozkoparan, Birsen
dc.contributor.departmentKUH (Koç University Hospital)
dc.contributor.departmentSchool of Medicine
dc.contributor.kuauthorŞahin, İrem Durmaz
dc.contributor.schoolcollegeinstituteKUH (KOÇ UNIVERSITY HOSPITAL)
dc.contributor.schoolcollegeinstituteSCHOOL OF MEDICINE
dc.date.accessioned2024-11-09T22:41:47Z
dc.date.issued2022
dc.description.abstractBackground: Although transplantation, surgical resection, and tumor ablation are treatment options available following early diagnosis of HCC, poor prognosis and high recurrence rates restrict the efficacy of these approaches. Hence, small molecules with high selectivity and bioactivity are urgently required. Objective: This study presents the synthesis of a series of new triazolothiadiazole derivatives (1a-3j) with NSAID moieties and their cytotoxic bioactivities. Methods: The new synthetic derivatives (1-3; 1a-3j) and NSAIDs ibuprofen, naproxen, and flurbiprofen that commonly used in clinics were screened against human liver (Huh7), breast (MCF7), and colon (HCT116) carcinoma cell lines under in vitro conditions via NCI-sulforhodamine B assay. Results: The 4-methoxyphenyl substituted condensed derivatives 1h, 2h, and 3h were the most active compounds. Based on its high potency, compound 3h was selected for the further biological evaluation of hepatocellular carcinoma cell lines, and the mechanisms underlying cell death induced by 3h were determined. The results revealed that compound 3h induced apoptosis and cell cycle arrest in the sub G1 phase in human liver cancer cells. Conclusion: These new small molecules may be used for the development of new lead compounds.
dc.description.indexedbyWOS
dc.description.indexedbyScopus
dc.description.indexedbyPubMed
dc.description.issue7
dc.description.openaccessNO
dc.description.publisherscopeInternational
dc.description.sponsoredbyTubitakEuN/A
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) [112S211] This project was funded by the Scientific and Technological Research Council of Turkey (TUBITAK) (Grant No: 112S211).
dc.description.volume22
dc.identifier.doi10.2174/1871520621666210623093550
dc.identifier.eissn1875-5992
dc.identifier.issn1871-5206
dc.identifier.quartileQ3
dc.identifier.scopus2-s2.0-85127457321
dc.identifier.urihttps://doi.org/10.2174/1871520621666210623093550
dc.identifier.urihttps://hdl.handle.net/20.500.14288/5995
dc.identifier.wos811705000013
dc.keywordsNovel Triazolothiadiazoles
dc.keywordsNSAIDs
dc.keywordsLiver Cancer
dc.keywordsCytotoxicity
dc.keywordsSRB
dc.keywordsAnticancer Nonsteroidal Antiinflammatory Drugs
dc.keywordsTriazolo-Thiadiazoles
dc.keywordsCancer Prevention
dc.keywordsCrystal-Structure
dc.keywordsDerivatives
dc.keywordsCytotoxicity
dc.keywordsAnalogs
dc.language.isoeng
dc.publisherBentham Science Publication Ltd
dc.relation.ispartofAnti-Cancer Agents in Medicinal Chemistry
dc.subjectOncology
dc.subjectPharmaceutical chemistry
dc.titleDesign, synthesis and biological evaluation of novel triazolothiadiazoles derived from NSAIDs as anticancer agents
dc.typeJournal Article
dspace.entity.typePublication
local.contributor.kuauthorŞahin, İrem Durmaz
local.publication.orgunit1SCHOOL OF MEDICINE
local.publication.orgunit1KUH (KOÇ UNIVERSITY HOSPITAL)
local.publication.orgunit2KUH (Koç University Hospital)
local.publication.orgunit2School of Medicine
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