New hydrazide-hydrazones and 1,3-thiazolidin-4-ones with 3-hydroxy-2-naphthoic moiety: Synthesis, in vitro and in vivo studies.

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ID: 104497
2018
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Ranked #24 of 39 articles by views in Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

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Abstract
In this research we synthesized, identified and evaluated new hydrazide-hydrazones (1-3) and 1,3-thiazolidin-4-one derivatives (4-6) for in vitro and in vivo activity. New hydrazide-hydrazones (1-3) were obtained by the condensation reaction of 3-hydroxy-2-naphthoic acid hydrazide with appropriate aldehydes. Synthesized hydrazide-hydrazones (1-3) were subjected to cyclization reaction with mercaptoacetic acid which afforded with new 1,3-thiazolidin-4-one derivatives (4-6). Among 1,3-thiazolidin-4-one derivatives tested (4-6), compound 6 exhibited highest and most selective cytotoxicity towards human renal adenocarcinoma cells (769-P) and it did not affect the growth of normal cells (H9c2, GMK). Whereas its hydrazide-hydrazone (compound 3) showed significant antiproliferative activity against both tested human cancer cell lines: renal adenocarcinoma (769-P) and hepatocellular carcinoma (HepG2), however with less selectivity. The in vivo studies focused on the antinociceptive activity of newly synthesized 1,3-thiazolidin-4-one derivatives (4-6). The preliminary screening of novel compounds showed that 1,3-thiazolidin-4-one derivatives (4-6) are safe and not toxic against CNS of mice. Among tested derivatives one compound (6) displayed significant analgesic activity.
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popioek2018newbiomedicine Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Popiołek, Łukasz;Piątkowska-Chmiel, Iwona;Gawrońska-Grzywacz, Monika;Biernasiuk, Anna;Izdebska, Magdalena;Herbet, Mariola;Sysa, Marcin;Malm, Anna;Dudka, Jarosław;Wujec, Monika;
Journal Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
Year 2018
DOI
S0753-3322(17)35472-0
URL
Keywords
Antimicrobial activity antiproliferative activity analgesic activity hydrazide-hydrazone 1,3-thiazolidin-4-one

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