Synthesis of vinca alkaloids and related compounds, Part XCVI. Nitration study of vinblastine-type bisindole alkaloids.
The bisindole alkaloids vinblastine, vincristine, and N-formyl-leurosine were nitrated and subsequently converted to amino derivatives. In the case of compounds 5e and 5b cytotoxic activity has been found for non-small cell lung cancer and breast cancer in the concentration range tested (10(-5)-10(-9) M). 5b also showed potency in the screen for colon cancer and leukemia.
Szabó
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Institute of Organic Chemistry, Budapest University of Technology and Economics, H-1111 Budapest, Gellért tér 4, Hungary.
Bölcskei
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Eszter
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Mák
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Szántay
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D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D001952:Bridged-Ring Compounds / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000737:chemistry; D007942:Leukemia, Experimental / Q000188:drug therapy / Q000401:mortality; D051379:Mice; D009584:Nitrogen; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014747:Vinblastine / Q000737:chemistry; D014748:Vinca Alkaloids / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D001952:Bridged-Ring Compounds; D007211:Indoles; D014748:Vinca Alkaloids; D014747:Vinblastine; D009584:Nitrogen