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Design, Synthesis, and Biological Evaluation of Combretabenzodiazepines: A Novel Class of Anti-Tubulin Agents

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Figshare2016-02-14 更新2026-04-29 收录
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In the present manuscript, starting from the 1,4-benzodiazepin-2-one nucleus, a privileged structure in medicinal chemistry, we have synthesized a novel class of cis-locked combretastatins named combreatabenzodiazepines. They show similar cytotoxic and antitubulin activity compared to combretastatin A-4 in neuroblastoma cells, showing a better pharmacokinetic profile. This class of compounds has therefore the potential for further development as antitubulin agents.

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2016-02-14
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