Abstract
A series of 2-triazenothiophene derivatives was prepared and tested to evaluate their biological activity. Two compounds inhibited the proliferation of leukemia, lymphoma and solid tumor-derived cell lines at micromolar concentrations, whereas none of the compounds were active against HIV-1. Compound 3c inhibited DNA, RNA and protein synthesis, and was also effective against KB cells resistant to etoposide and vincristine. The compounds were inactive against fungi and bacteria.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Bacterial Agents
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Anti-HIV Agents / pharmacology
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Anti-Infective Agents / pharmacology
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Bacteria / drug effects
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Carcinoma / pathology
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Cytopathogenic Effect, Viral / drug effects
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Drug Evaluation, Preclinical
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Drug Resistance, Neoplasm
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Drug Screening Assays, Antitumor
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Fungi / drug effects
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HIV-1 / drug effects
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HeLa Cells / drug effects
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Humans
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KB Cells / drug effects
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Leukemia / pathology
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Lymphoma / pathology
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Melanoma / pathology
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Structure-Activity Relationship
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Thiophenes / chemical synthesis
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Thiophenes / pharmacology*
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Triazenes / chemical synthesis
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Triazenes / pharmacology*
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Tumor Cells, Cultured / drug effects
Substances
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Anti-Bacterial Agents
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Anti-HIV Agents
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Anti-Infective Agents
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Antineoplastic Agents
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Thiophenes
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Triazenes