Publication: Design, synthesis and biological evaluation of novel triazolothiadiazoles derived from NSAIDs as anticancer agents
dc.contributor.coauthor | Aytaç, Peri | |
dc.contributor.coauthor | Atalay, Rengül Çetin | |
dc.contributor.coauthor | Tozkoparan, Birsen | |
dc.contributor.department | KUH (Koç University Hospital) | |
dc.contributor.department | School of Medicine | |
dc.contributor.kuauthor | Şahin, İrem Durmaz | |
dc.contributor.schoolcollegeinstitute | KUH (KOÇ UNIVERSITY HOSPITAL) | |
dc.contributor.schoolcollegeinstitute | SCHOOL OF MEDICINE | |
dc.date.accessioned | 2024-11-09T22:41:47Z | |
dc.date.issued | 2022 | |
dc.description.abstract | Background: 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.indexedby | WOS | |
dc.description.indexedby | Scopus | |
dc.description.indexedby | PubMed | |
dc.description.issue | 7 | |
dc.description.openaccess | NO | |
dc.description.publisherscope | International | |
dc.description.sponsoredbyTubitakEu | N/A | |
dc.description.sponsorship | Scientific 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.volume | 22 | |
dc.identifier.doi | 10.2174/1871520621666210623093550 | |
dc.identifier.eissn | 1875-5992 | |
dc.identifier.issn | 1871-5206 | |
dc.identifier.quartile | Q3 | |
dc.identifier.scopus | 2-s2.0-85127457321 | |
dc.identifier.uri | https://doi.org/10.2174/1871520621666210623093550 | |
dc.identifier.uri | https://hdl.handle.net/20.500.14288/5995 | |
dc.identifier.wos | 811705000013 | |
dc.keywords | Novel Triazolothiadiazoles | |
dc.keywords | NSAIDs | |
dc.keywords | Liver Cancer | |
dc.keywords | Cytotoxicity | |
dc.keywords | SRB | |
dc.keywords | Anticancer Nonsteroidal Antiinflammatory Drugs | |
dc.keywords | Triazolo-Thiadiazoles | |
dc.keywords | Cancer Prevention | |
dc.keywords | Crystal-Structure | |
dc.keywords | Derivatives | |
dc.keywords | Cytotoxicity | |
dc.keywords | Analogs | |
dc.language.iso | eng | |
dc.publisher | Bentham Science Publication Ltd | |
dc.relation.ispartof | Anti-Cancer Agents in Medicinal Chemistry | |
dc.subject | Oncology | |
dc.subject | Pharmaceutical chemistry | |
dc.title | Design, synthesis and biological evaluation of novel triazolothiadiazoles derived from NSAIDs as anticancer agents | |
dc.type | Journal Article | |
dspace.entity.type | Publication | |
local.contributor.kuauthor | Şahin, İrem Durmaz | |
local.publication.orgunit1 | SCHOOL OF MEDICINE | |
local.publication.orgunit1 | KUH (KOÇ UNIVERSITY HOSPITAL) | |
local.publication.orgunit2 | KUH (Koç University Hospital) | |
local.publication.orgunit2 | School of Medicine | |
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