RUI: Synthesis of New Furanosteroids Related to Wortmannin

在这个由化学系化学合成计划资助的项目中，福尔曼大学化学系的Brian C.Goess教授将开发倍半萜呋喃类固醇天然产物家族新成员的合成。这些分子，包括Wortmannin，由于它们能够抑制磷脂酰肌醇-3-激酶(PI3K)而引起了人们的极大关注，PI3K是已知在细胞生长和分化中发挥关键作用的酶。将开发这一系列天然产品中六个新成员的合成，这些成员以前都没有合成过。此外，对合成路线的修改将产生适合用于测定这些新天然产物的生物活性的类似物。这些新天然产物仅从其自然来源中分离出微量。鉴于它们的重要生物活性和作为化疗药物的潜力，这些分子中的每一个都需要进行化学合成。这项工作还将使更有效的方法来制备整个分子家族，包括那些存在但尚未从自然来源中分离出来的分子。该项目可能会对制药行业和普通生物学研究产生重大影响。这个项目还将作为本科生化学家的培训基地，他们中的许多人将进入化学研究生院，在那里他们在这个项目中发展的技能将得到广泛应用。

In this project funded by the Chemical Synthesis program of the Chemistry Division, Professor Brian C. Goess of the Department of Chemistry at Furman University will develop syntheses of new members of the sesquiterpene furanosteroid family of natural products. These molecules, which include wortmannin, have attracted significant attention for their ability to inhibit the phosphatidylinositol-3-kinases (PI3K), enzymes known to play a critical role in cell growth and differentiation. Syntheses of six new members of this family of natural products, none of which have been previously synthesized, will be developed. Additionally, modifications to the synthesis routes will generate analogs suitable for use in assays to determine the biological activities of these new natural products.These new natural products are isolated in only minute quantities from their natural sources. Given their important biological activities and their potential as chemotherapeutics, chemical synthesis of each of these molecules is necessary. This work will also enable more efficient methods for the preparation of this entire family of molecules, including those that exist but have not yet been isolated from natural sources. This project could have significant impacts on pharmaceutical industries and general biological studies. This project will also serve as the training ground for undergraduate chemists, many of which will attend graduate schools in chemistry, where the skills they develop on this project will be extensively utilized.