Synthesis, Biological Evaluation and Ligand Based Pharmacophore Modeling of New Aromatic Thiosemicarbazones as Potential Anticancer Agents
Identifieur interne : 000D16 ( Main/Exploration ); précédent : 000D15; suivant : 000D17Synthesis, Biological Evaluation and Ligand Based Pharmacophore Modeling of New Aromatic Thiosemicarbazones as Potential Anticancer Agents
Auteurs : A. Karaküçük- Yido An [Turquie] ; B. Ayd Nöz [Turquie] ; T. Ta K N-Tok [Turquie] ; E. E. Oruç-Emre [Turquie] ; J. Balzarini [Belgique]Source :
- Pharmaceutical Chemistry Journal [ 0091-150X ] ; 2019.
Abstract
Two series of new aromatic thiosemicarbazone derivatives were synthesized by condensation of
Url:
DOI: 10.1007/s11094-019-01968-3
PubMed: NONE
PubMed Central: 7089137
Affiliations:
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Le document en format XML
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<author><name sortKey="Karakucuk Yido An, A" sort="Karakucuk Yido An, A" uniqKey="Karakucuk Yido An A" first="A." last="Karaküçük- Yido An">A. Karaküçük- Yido An</name>
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27310 Gaziantep, Turkey</nlm:aff>
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<author><name sortKey="Ayd Noz, B" sort="Ayd Noz, B" uniqKey="Ayd Noz B" first="B." last="Ayd Nöz">B. Ayd Nöz</name>
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27310 Gaziantep, Turkey</nlm:aff>
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<series><title level="j">Pharmaceutical Chemistry Journal</title>
<idno type="ISSN">0091-150X</idno>
<idno type="eISSN">1573-9031</idno>
<imprint><date when="2019">2019</date>
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<front><div type="abstract" xml:lang="en"><p id="Par1">Two series of new aromatic thiosemicarbazone derivatives were synthesized by condensation of <italic>N</italic>
-(4-cyanophenyl)hydrazine carbothioamide (<bold>I</bold>
) and <italic>N</italic>
-(4-methylsulfanylphenyl)hydrazine carbothioamide (<bold>II</bold>
) with appropriate aromatic aldehydes in order to investigate their antiviral and cytostatic potency. The chemical structures of all compounds were fully characterized by elemental analysis and spectroscopic techniques. The results of the bioassays indicated that compounds <bold>Id</bold>
, <bold>Ie</bold>
, <bold>If</bold>
and <bold>IIf</bold>
proved inhibitory against influenza virus A (EC<sub>50</sub>
= 13 – 27 μg/mL for strain H1N1 and 9.3 – 18 μg/mL for strain H3N2). Compounds <bold>Ig</bold>
and <bold>IIg</bold>
were the most cytostatic compounds with inhibition of HeLa cell proliferation at an IC<sub>50</sub>
= 0.3 μg/mL for <bold>Ig</bold>
and 1.9 μg/mL for <bold>IIg</bold>
. Especially, compound <bold>Ig</bold>
showed the highest cytostatic activity with IC<sub>50</sub>
of 0.30, 0.70 and 2.50 μg/mL against HeLa, CEM and L1210 cell lines, respectively. This inhibition range was within the same order of magnitude as that for cisplatin. Furthermore, molecular modeling was carried out to examine the cytostatic activity and determine the best pharmacophore model as a guide for the design and development of potential prodrugs in future studies.</p>
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