title: Synthesis and antitumor activity of inositol phosphotriester analogues.
abstract: Inositol phosphates, as important second messengers of signal transduction, regulate many biological functions. However, cell penetration and phospholipase stability could be two main issues faced by inositol phosphate analogues used as lead compounds for drug discovery. Inositol phosphotriester analogues could be more beneficial to diffuse across plasma membrane. In this paper, we describe the design and synthesis of a series of inositol phosphotriester analogues based on phosphatidylinositol, along with the initial antitumor activity analysis. Several compounds exhibited good cytotoxic activity against human cancer cell lines A549, HepG2, MDA-MB-231 and HeLa, especially compound 33 was cytotoxic against all the four cancer cell lines with good IC(50) values.
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry and Department of Chemical Biology, Nankai University, Tianjin, China.
authors.forename: Fanbo
authors.initials: F
authors.lastname: Song
authors.forename: Jing
authors.initials: J
authors.lastname: Zhang
authors.forename: Yuefang
authors.initials: Y
authors.lastname: Zhao
authors.forename: Wenbin
authors.initials: W
authors.lastname: Chen
authors.forename: Luyuan
authors.initials: L
authors.lastname: Li
authors.forename: Zhen
authors.initials: Z
authors.lastname: Xi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001940:Breast / Q000166:cytology / Q000187:drug effects; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D004354:Drug Screening Assays, Antitumor; D004847:Epithelial Cells / Q000187:drug effects; D005260:Female; D006367:HeLa Cells; D006801:Humans; D007295:Inositol Phosphates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007295:Inositol Phosphates