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Abstract
Three types of novel triptolide analogues with 9,11-olefin ( 3– 5), five-membered unsaturated lactam ring ( 6– 7) or A/B cis ring junction ( 8– 14) were synthesized. Although with 9,11-olefin instead of 9,11-β-epoxide, compound 4a was much more active than the parent natural triptolide ( 1) with the lowest IC 50 value of 0.05 nM for SKOV-3 cells, clearly challenging the traditional viewpoint on the necessity of 9,11-β-epoxide group of triptolide. In addition, structure–activity relationships for three classes of compounds were studied.
Published Version
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