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.
Derivatives of 2-aminothiophene-3-carbonitrile, 2-thioxopyridine-3-carbonitrile, 1,8-naphthyridine-2one, thieno[2,3-b]pyridine-5-carbonitrile and thieno[2,3-d]pyrimidine incorporating with a 1H-b e n z otriazole moiety or 1,3,4-thiadiazole derivatives incorporating with a benzotriazol-1-ylmethyl group have been synthesized and tested for antimicrobial and antifungal activities. The structures of the newly synthesized compounds have been established on the basis of their analytical and spectral data. Pharmacological studies of the 1H-b e n z o t r i a z o l e nucleus have been shown to posses a variety of pharmacological activities such as anti-inflammatory [1], antimicrobial [2-4], anticonvulsant and CNS depressant [5] effects. Furthermore, several pharmacological studies have also pointed out the value of 2-aminothiophene [6,7], naphthyridine [8], thieno[2,3-d]pyrimidine [9,10], thieno[2,3b]pyridine [11] and thiadiazole [12] as biologically active nuclei. These findings focused on incorporating 2aminothiophene-3-carbonitrile, 2-thioxopyridine-3-carbonitrile, 4-amino-2-oxo-1,8-naphthyridine-3-carbonitrile, 4 -a m i n o t h i e n o [ 2 , 3 -b]pyridine-5-carbonitrile and thieno[2,3-d] pyrimidine with 1H
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