Synthesis and antiproliferative activity of 2-triazenothiophenes.
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.
Diana
P
P
Istituto Farmacochimico, Università degli Studi, Palermo, Italy.
Barraja
P
P
Lauria
A
A
Almerico
A M
AM
Cirrincione
G
G
Minnei
C
C
Longu
S
S
Congiu
D
D
Musiu
C
C
La Colla
P
P
D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002277:Carcinoma / Q000473:pathology; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D005658:Fungi / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D007624:KB Cells / Q000187:drug effects; D007938:Leukemia / Q000473:pathology; D008223:Lymphoma / Q000473:pathology; D008545:Melanoma / Q000473:pathology; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology*; D014226:Triazenes / Q000138:chemical synthesis / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D013876:Thiophenes; D014226:Triazenes