Wender Paul A, Dechristopher Brian A, Schrier Adam J
Departments of Chemistry and Chemical and Systems Biology, Stanford University, Stanford, California 94305-5080, USA.
J Am Chem Soc. 2008 May 28;130(21):6658-9. doi: 10.1021/ja8015632. Epub 2008 May 2.
The step-economical synthesis of a new class of bryostatin analogues that contain the complete oxycarbocyclic core ring system of the bryostatin natural products is reported. These agents are convergently assembled via a highly efficient, functional-group-tolerant, and stereoselective Prins-driven macrocyclization. These tetrahydropyranyl B-ring analogues are among our most potent and efficacious analogues to date, exhibiting nanomolar and picomolar activities in protein kinase C affinity assays as well as in cellular antiproliferation assays.
报道了一类新型苔藓抑素类似物的逐步经济合成方法,该类似物含有苔藓抑素天然产物完整的氧碳环核心环系统。这些化合物通过高效、官能团耐受性和立体选择性的普林斯驱动大环化反应进行汇聚组装。这些四氢吡喃基B环类似物是我们迄今为止最有效和最具活性的类似物之一,在蛋白激酶C亲和力测定以及细胞抗增殖测定中表现出纳摩尔和皮摩尔活性。