Abstract
A series of 3- and 5-methylthiophene-2-carboxaldehyde alpha-(N)-heterocyclichydrazones were synthesized and submitted to an in vitro investigation of their anticancer, anti-HIV and antimicrobial activities. Some of the newly synthesized compounds were found to possess antiproliferative properties, whereas no anti-HIV activity was seen; the most active of the series was the derivative 2i, which exhibited tumour growth inhibition activity against all cell lines displaying GI50 values between 1.63 and 26.5 microM. The title compounds were generally ineffective against Gram-positive and Gram-negative bacteria, while showed a moderate antifungal activity against C. albicans and A. fumigatus.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / pharmacology*
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / pharmacology*
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Antifungal Agents / chemical synthesis
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Antifungal Agents / pharmacology
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Cell Division / drug effects
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Cell Line, Tumor
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Drug Evaluation, Preclinical / methods
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Drug Screening Assays, Antitumor
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Gram-Negative Bacteria / drug effects
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Gram-Positive Bacteria / drug effects
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Humans
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Hydrazones / chemical synthesis
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Hydrazones / pharmacology*
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Microbial Sensitivity Tests
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Molecular Structure
Substances
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Anti-Bacterial Agents
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Anti-HIV Agents
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Antifungal Agents
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Antineoplastic Agents
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Hydrazones