New hydrazide-hydrazones and 1,3-thiazolidin-4-ones with 3-hydroxy-2-naphthoic moiety: Synthesis, in vitro and in vivo studies - 29/05/18
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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.
El texto completo de este artículo está disponible en PDF.Keywords : Hydrazide-hydrazone, 1,3-Thiazolidin-4-one, Antiproliferative activity, Analgesic activity, Antimicrobial activity
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Vol 103
P. 1337-1347 - juillet 2018 Regresar al númeroBienvenido a EM-consulte, la referencia de los profesionales de la salud.
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