Synthesis and preliminary mechanistic evaluation of 5-(p-tolyl)-1-(quinolin-2-yl)pyrazole-3-carboxylic acid amides with potent antiproliferative activity on human cancer cell lines

Simple item page
buir.contributor.authorDurmaz, İrem
buir.contributor.authorAtalay, Rengül
dc.citation.epage149en_US
dc.citation.spage140en_US
dc.citation.volumeNumber87en_US
dc.contributor.authorCankara-Pirol, Ş.en_US
dc.contributor.authorÇalışkan, B.en_US
dc.contributor.authorDurmaz, İremen_US
dc.contributor.authorAtalay, Rengülen_US
dc.contributor.authorBanoğlu, E.en_US
dc.date.accessioned2016-02-08T10:36:28Z
dc.date.available2016-02-08T10:36:28Z
dc.date.issued2014en_US
dc.departmentDepartment of Molecular Biology and Geneticsen_US
dc.departmentGenetics and Biotechnology Research Center (BİLGEN)en_US
dc.description.abstractWe synthesized a series of novel amide derivatives of 5-(p-tolyl)-1-(quinolin-2-yl)pyrazole-3-carboxylic acid and assessed their antiproliferative activities against three human cancer cell lines (Huh7, human liver; MCF7, breast and HCT116, colon carcinoma cell lines) with the sulforhodamine B assay. Compound 4j with 2-chloro-4-pyridinyl group in the amide part exhibited promising cytotoxic activity against all cell lines with IC<inf>50</inf>values of 1.6 μM, 3.3 μM and 1.1 μM for Huh7, MCF7 and HCT116 cells, respectively, and produced dramatic cell cycle arrest at SubG1/G1 phase as an indicator of apoptotic cell death induction. On the basis of their high potency in cellular environment, these straightforward pyrazole-3-carboxamide derivatives may possess potential in the design of more potent compounds for intervention with cancer cell proliferation.en_US
dc.identifier.doi10.1016/j.ejmech.2014.09.056en_US
dc.identifier.issn0223-5234
dc.identifier.urihttp://hdl.handle.net/11693/24936
dc.language.isoEnglishen_US
dc.publisherElsevieren_US
dc.relation.isversionofhttps://doi.org/10.1016/j.ejmech.2014.09.056en_US
dc.source.titleEuropean Journal of Medicinal Chemistryen_US
dc.subjectApoptosisen_US
dc.subjectAutophagyen_US
dc.subjectCytotoxicityen_US
dc.subjectDiarylpyrazoleen_US
dc.subjectQuinolineen_US
dc.subjectG1 phaseen_US
dc.titleSynthesis and preliminary mechanistic evaluation of 5-(p-tolyl)-1-(quinolin-2-yl)pyrazole-3-carboxylic acid amides with potent antiproliferative activity on human cancer cell linesen_US
dc.typeArticleen_US

Files

Original bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
Synthesis and preliminary mechanistic evaluation of 5-(p-tolyl)-1-(quinolin-2-yl)pyrazole-3-carboxylic acid amides with potent antiproliferative activity on human cancer cell lines.pdf
Size:
1.44 MB
Format:
Adobe Portable Document Format
Description:
Full printable version
Download

Collections

Department of Molecular Biology and Genetics
Genetics and Biotechnology Research Center (BİLGEN)