Novel synthesis of hydrazide-hydrazone derivatives and their utilization in the synthesis of coumarin, pyridine, thiazole and thiophene derivatives with antitumor activity

Mohareb R.M.; Fleita D.H.; Sakka O.K.

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Novel synthesis of hydrazide-hydrazone derivatives and their utilization in the synthesis of coumarin, pyridine, thiazole and thiophene derivatives with antitumor activity

Mohareb R.M.; Fleita D.H.; Sakka O.K.

Full Text link: https://t.ly/ge8P2

Date issued: 2011

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Doi: https://doi.org/10.3390/molecules16010016 PubMed ID 21187814

Series Info: Molecules
16

Type: Article

Keywords: 3-acetylpyridine , Antitumor activity , Coumarin , Hydrazide-hydrazone , Thiophene , antineoplastic agent , azide , coumarin , coumarin derivative , hydrazone derivative , pyridine , pyridine derivative , thiazole derivative , thiophene derivative , article , cell division , chemistry , drug effect , drug screening , human , nuclear magnetic resonance spectroscopy , tumor cell line , Antineoplastic Agents , Azides , Cell Division , Cell Line, Tumor , Coumarins , Drug Screening Assays, Antitumor , Humans , Hydrazones , Magnetic Resonance Spectroscopy , Pyridines , Thiazoles , Thiophenes

Abstract:

The reaction of cyanoacetyl hydrazine (1) with 3-acetylpyridine (2) gave the hydrazide-hydrazone derivative 3. The latter compound undergoes a series of heterocyclization reactions to give new heterocyclic compounds. The antitumor evaluation of the newly synthesized products against three cancer cell lines, namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) was performed. Most of the synthesized compounds showed high inhibitory effects. � 2010 by the authors.