Abstract
Several 8-chloro-7-R1-6-R2-3-R3-imidazo[1,2-b][1,4,2]benzodithiazine 5,5-dioxide derivatives (9-11, 16-19, and 21-24) have been synthesized as potential antitumor or anti-HIV agents. The in vitro antitumor and anti-HIV-1 activities of the compounds were determined in a panel of cell lines. The benzodithiazine-dioxide 10 showed 50% growth inhibitory activity in low micromolar against most cells. It was particularly effective in leukemia, lung, melanoma, ovarian, and renal cancer cells with GI50 values of 1-2 microM. Interestingly, benzodithiazine-dioxide 16 showed remarkable anti-HIV-1 activity with 50% effective concentration EC50 value of 0.94 microM and no significant cytotoxicity at 200.0 microM.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anhydrides / chemistry
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Anti-HIV Agents / chemical synthesis*
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacology*
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Chlorine / chemistry
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Drug Evaluation, Preclinical
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Esters / chemistry
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HIV-1 / drug effects
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Humans
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Imidazoles / chemistry
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Methylation
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Molecular Structure
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Oxygen / chemistry*
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Structure-Activity Relationship
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Thiazines / chemical synthesis
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Thiazines / chemistry*
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Thiazines / pharmacology*
Substances
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Anhydrides
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Anti-HIV Agents
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Antineoplastic Agents
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Esters
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Imidazoles
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Thiazines
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Chlorine
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imidazole
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Oxygen