毒胡萝卜素的合成。
Synthesis of the thapsigargins.
作者信息
Ley Steven V, Antonello Alessandra, Balskus Emily P, Booth David T, Christensen Søren B, Cleator Ed, Gold Helen, Högenauer Klemens, Hünger Udo, Myers Rebecca M, Oliver Steven F, Simic Oliver, Smith Martin D, Søhoel Helmer, Woolford Alison J A
机构信息
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, United Kingdom.
出版信息
Proc Natl Acad Sci U S A. 2004 Aug 17;101(33):12073-8. doi: 10.1073/pnas.0403300101. Epub 2004 Jun 28.
Abstract
The thapsigargins are a family of complex guaianolides with potent and selective Ca(2+)-modulating properties. This article documents the evolution of a synthetic route through several iterations to a final practical and scaleable synthetic route capable of generating both unnatural and natural products based around the guaianolide skeleton.
摘要
毒胡萝卜内酯是一类具有强效且选择性钙调节特性的复杂愈创木烷型倍半萜内酯。本文记录了一条合成路线经过多次迭代演变成最终实用且可规模化的合成路线的过程，该路线能够基于愈创木烷型倍半萜内酯骨架生成非天然产物和天然产物。
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本文引用的文献
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Synthesis and Biological Activity of Sarcodictyins.肉珊瑚素的合成与生物活性
Angew Chem Int Ed Engl. 1998 Jun 5;37(10):1418-1421. doi: 10.1002/(SICI)1521-3773(19980605)37:10<1418::AID-ANIE1418>3.0.CO;2-5.
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A route to the thapsigargins from (S)-carvone providing a substrate-controlled total synthesis of trilobolide, nortrilobolide, and thapsivillosin F.一条从（S）-香芹酮合成毒胡萝卜内酯的路线，实现了三叶内酯、去甲三叶内酯和毒胡萝卜素F的底物控制全合成。
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Prostate-specific antigen-activated thapsigargin prodrug as targeted therapy for prostate cancer.前列腺特异性抗原激活的毒胡萝卜素前药作为前列腺癌的靶向治疗
J Natl Cancer Inst. 2003 Jul 2;95(13):990-1000. doi: 10.1093/jnci/95.13.990.
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Design, synthesis, and pharmacological evaluation of thapsigargin analogues for targeting apoptosis to prostatic cancer cells.靶向前列腺癌细胞凋亡的毒胡萝卜素类似物的设计、合成及药理评价
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Thapsigargin analogues for targeting programmed death of androgen-independent prostate cancer cells.用于靶向雄激素非依赖性前列腺癌细胞程序性死亡的毒胡萝卜素类似物。
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A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca(2+)-ATPases.一种成熟的工具：毒胡萝卜素作为肌浆网/内质网Ca(2+) -ATP酶的抑制剂
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Sesquiterpenoids from Thapsia species and medicinal chemistry of the thapsigargins.
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Thapsigargin discriminates strongly between Ca(2+)-ATPase phosphorylated intermediates with different subcellular distributions in bovine adrenal chromaffin cells.
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Thapsigargin inhibits the sarcoplasmic or endoplasmic reticulum Ca-ATPase family of calcium pumps.毒胡萝卜素抑制肌浆网或内质网钙泵的钙ATP酶家族。
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