9. Synthesis of Chamaecypanone C Analogues from in Situ-Generated Cyclopentadienones and Their Biological Evaluation
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作者:Suwei Dong, Tian Qin, Ernest Hamel, John A. Beutler, and John A. Porco, Jr.*
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发布时间: 2012-10-31
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J. Am. Chem. Soc. 2012, 134, 19782-19787.
Suwei Dong, Tian Qin, Ernest Hamel, John A. Beutler, and John A. Porco, Jr.*
A rhodium-catalyzed dehydrogenation protocol for the conversion of 3,5-diarylcyclopentenones to the corresponding 2,4-diarylcyclopentadienones has been developed. With this protocol, analogues of the cytotoxic agent chamaecypanone C have been synthesized via Diels–Alder cycloaddition between the cyclopentadienones and in suit-generated O-quinols. Biological evaluation of these analogues revealed a compound with higher activity as a microtubule inhibitor and cytotoxic agent in comparison with the parent structure.
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