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Bioorg Med Chem Lett ; 9(2): 145-50, 1999 Jan 18.
Article in English | MEDLINE | ID: mdl-10021917

ABSTRACT

All four "symmetrical" regioisomers of ED-110, an indolocarbazole derivative having potent activity against human topoisomerase I (Topo I) were synthesized. The isomer containing hydroxyl groups in the 3- and 9-positions was approximately ten-fold more active against Topo I, and 5- to 35-fold more active against human solid tumor cell lines in vitro, relative to ED-110.


Subject(s)
Carbazoles/pharmacology , Glucosides/pharmacology , Topoisomerase I Inhibitors , Antineoplastic Agents , Camptothecin/pharmacology , Carbazoles/chemical synthesis , Female , Glucosides/chemical synthesis , HT29 Cells , Humans , Inhibitory Concentration 50 , Male , Ovarian Neoplasms/drug therapy , Prostatic Neoplasms/drug therapy , Tumor Cells, Cultured
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