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Updated: May 22, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Total Syntheses of Plocabulin and Its C2-Analogues
Shunfa Liu1, Bin Li1, Xin Gao1
1Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, China.
Abstract:
Plocabulin is a structurally unique marine natural product with potent antitumor activity, making it a promising candidate for the development of antibody-drug conjugates (ADCs). However, its extremely low natural abundance has limited further research and therapeutic exploration. In this study, we present a convergent synthetic strategy for plocabulin and its C2-analogues. Our approach enabled the synthesis of 1.23 g of plocabulin through a longest linear sequence of 12 steps and a total of 24 steps, achieving an overall yield of 19.7%.
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