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pubmed-article:19254843pubmed:abstractTextNovel hexacyclic camptothecin analogs containing cyclic amidine, urea, or thiourea moiety were designed and synthesized based on the proposed 3D-structure of the topoisomerase I (Topo I)/DNA/camptothecin ternary complex. The analogs were prepared from 9-nitrocamptothecin via 7,9-diaminocamptothecin derivatives as a key intermediate. Among them, 7c exhibited in vivo antitumor activities superior to CPT-11 in human cancer xenograft models in mice at their maximum tolerated doses though its in vitro antiproliferative activity was comparable to SN-38 against corresponding cell lines.lld:pubmed
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pubmed-article:19254843pubmed:dateRevised2010-11-18lld:pubmed
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pubmed-article:19254843pubmed:articleTitleSynthesis of new camptothecin analogs with improved antitumor activities.lld:pubmed
pubmed-article:19254843pubmed:affiliationKamakura Research Laboratories, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan.lld:pubmed
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