Synthesis and evaluation of the antitumor activity of Calix[4]arene L-proline derivatives

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dc.contributor.authorOguz, Mehmet.
dc.contributor.authorGul, Alev.
dc.contributor.authorKarakurt, Serdar.
dc.contributor.authorYilmaz, Mustafa.
dc.date.accessioned2020-03-26T20:20:30Z
dc.date.available2020-03-26T20:20:30Z
dc.date.issued2020
dc.departmentSelçuk Üniversitesi, Fen Fakültesi, Kimya Bölümüen_US
dc.description.abstractThe unique conformational properties, functionality, low toxicity, and low cost make calixarene-based compounds a valuable candidate against cancer. The aim of the present study is the synthesis of the upper rim and lower rim-functionalized L-proline-based calix[4]arene derivatives and evaluation of their cytotoxic potential for human cancerous cells as well as to determine the death mechanism. Synthesized calix[4]arene (3, 8a, 8b 13a, and 13b) derivatives were characterized by different spectroscopic techniques such as (HNMR)-H-1, (CNMR)-C-13, and FTIR. In vitro effects of compounds 3, 8a, 8b, 13a and 13b were tested on human cancerous cells (HEPG2, PC-3, A-549, and DLD-1) as well as human healthy epithelium cell (PNT1A). Results show that compounds 3, 8a, 8b and 13b have cytotoxic potential on human colorectal carcinoma cells (DLD-1) with IC50, values of 43 mu M, 45.2 mu M, 64.57 mu M, and 29.35 mu M respectively. Apoptosis ratios of cell death were investigated with flow cytometer using 7-AAD and Annexin-V as markers. Cytotoxic potential of 8a was found to be higher due to increased apoptosis, when compared with healthy cells the apoptotic cell death was significantly (p < 0.0001) increased up to 1.7-fold and 2.4-fold in DLD-1 and A549 cells, respectively. In conclusion, these L-proline derived calix[4]arenes with their selective cytotoxic potential on human cancerous cells may be a potential candidate for the treatment of human CRC and lung cancer.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey, Turkey (TUBITAK-Grant) [116Z173]; Research Foundation of Selcuk UniversitySelcuk University [17201066, 17201064]en_US
dc.description.sponsorshipWe would like to thank the Scientific and Technological Research Council of Turkey, Turkey (TUBITAK-Grant Number 116Z173) and the Research Foundation of Selcuk University (SUBAP-Grant Number: 17201066 and 17201064) for financial support of this work and is a part of Mehmet Oguz Ph.D. thesis and Alev Gul master thesis.en_US
dc.identifier.citationOguz, M., Gul, A., Karakurt, S., Yilmaz, M. (2020). Synthesis and Evaluation of the Antitumor Activity of Calix[4]arene L-proline Derivatives. Bioorganic Chemistry, 94, 1-8.
dc.identifier.doi10.1016/j.bioorg.2019.103207en_US
dc.identifier.issn0045-2068en_US
dc.identifier.issn1090-2120en_US
dc.identifier.pmid31451296en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://dx.doi.org/10.1016/j.bioorg.2019.103207
dc.identifier.urihttps://hdl.handle.net/20.500.12395/38601
dc.identifier.volume94en_US
dc.identifier.wosWOS:000505596300002en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorOguz, Mehmet.
dc.institutionauthorGul, Alev.
dc.institutionauthorKarakurt, Serdar.
dc.institutionauthorYilmaz, Mustafa.
dc.language.isoenen_US
dc.publisherACADEMIC PRESS INC ELSEVIER SCIENCEen_US
dc.relation.ispartofBIOORGANIC CHEMISTRYen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.selcuk20240510_oaigen_US
dc.subjectCalixareneen_US
dc.subjectL-Prolineen_US
dc.subjectCytotoxicityen_US
dc.subjectApoptosisen_US
dc.subjectAnticancer agenten_US
dc.titleSynthesis and evaluation of the antitumor activity of Calix[4]arene L-proline derivativesen_US
dc.typeArticleen_US

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