RUI: Synthesis of New Furanosteroids Related to Wortmannin

RUI：与渥曼青霉素相关的新型呋喃类固醇的合成

• 批准号: 1213569
• 负责人: Brian Goess
• 金额: $ 19.92万
• 依托单位: Furman University
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2012
• 资助国家: 美国
• 起止时间: 2012-09-01 至 2016-08-31
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1213569&HistoricalAwards=false
• 关键词: RUI; Synthesis; New; Furanosteroids; Related

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.

在这个由化学系化学合成项目资助的项目中，Brian C.弗曼大学化学系的Goess将开发合成倍半萜呋喃甾类天然产物家族的新成员。 这些分子，包括渥曼青霉素，由于其抑制磷脂酰肌醇-3-激酶（PI 3 K）的能力而引起了人们的极大关注，磷脂酰肌醇-3-激酶（PI 3 K）是已知在细胞生长和分化中起关键作用的酶。 将开发这个天然产物家族的六个新成员的合成，其中没有一个是以前合成的。 此外，对合成路线的修改将产生适用于测定这些新天然产物的生物活性的类似物。 鉴于它们重要的生物活性和它们作为化学治疗剂的潜力，这些分子中的每一个的化学合成是必要的。 这项工作也将使更有效的方法来制备这整个家族的分子，包括那些存在的，但尚未从天然来源分离。 该项目可能对制药工业和一般生物学研究产生重大影响。 该项目还将作为本科化学家的培训基地，其中许多人将参加化学研究生院，他们在该项目上开发的技能将得到广泛利用。