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Design, synthesis, cytotoxic activity and molecular docking studies of new 20(S)-sulfonylamidine camptothecin derivatives
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文摘

20(S)-Sulfonylamidine CPT-derivatives were prepared and tested for cytotoxicity.

Several analogs showed superior cytotoxic activity compared to irinotecan.

Key structural features related to cytotoxicity were identified by SAR analysis.

Compounds rong class="boldFont">9rong> and rong class="boldFont">15crong> interacted with Topo I-DNA by a different binding mode from CPT.

These compounds are new generation CPT-derived antitumor agents.

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