title: Synthesis of Pelorol and Its Analogs and Their Inhibitory Effects on Phosphatidylinositol 3-Kinase.
abstract: There are numerous biologically active substances with novel structures and unique physiological functions in marine organisms. These substances are important sources of new lead compounds. Pelorol is a natural product isolated from marine organisms that possesses a novel structure with high bioactivity. In this paper, the synthesis of pelorol has been completed, and the synthesis of some intermediates has been optimized and scaled up. Five pelorol analogs have also been prepared. Preliminary biological activity testing demonstrated that compounds 5 and 6 might be potential lead compounds for cancer therapy.
authors.affiliation: Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. 18666353586@163.com.
authors.forename: Yongjie
authors.initials: Y
authors.lastname: Luo
authors.affiliation: Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. chenhx33@mail2.sysu.edu.cn.
authors.forename: Huixuan
authors.initials: H
authors.lastname: Chen
authors.affiliation: Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. wengj2@mail.sysu.edu.cn.
authors.forename: Jiang
authors.initials: J
authors.lastname: Weng
authors.affiliation: Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. lugui@mail.sysu.edu.cn.|Institute of Human Virology, Sun Yat-sen University, Guangzhou 510080, China. lugui@mail.sysu.edu.cn.
authors.forename: Gui
authors.initials: G
authors.lastname: Lu
mesh_terms: D059001:Aquatic Organisms / Q000737:chemistry; D001688:Biological Products / Q000737:chemistry* / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D020014:K562 Cells; D061986:MCF-7 Cells; D000081082:Phosphoinositide-3 Kinase Inhibitors; D012717:Sesquiterpenes / Q000737:chemistry* / Q000494:pharmacology*; D020298:U937 Cells
chemical_list: D001688:Biological Products; D000081082:Phosphoinositide-3 Kinase Inhibitors; D012717:Sesquiterpenes; C414692:pelorol
keywords: PI3K inhibitor; anti-tumor activity; marine organisms; pelorol; total synthesis