title: Recent advances in the synthesis of tubulysins.
abstract: Tubulysins are a family of natural tetrapeptides in clinical development as a consequence of their potent anticancer activity, even for multi-drug resistant carcinoma. Tubulysins inhibit tubulin polymerization by binding to the peptide binding site located near the vinca alkaloid binding site of tubulin. The limited availability and pharmacological profile of the tubulysins attracted synthetic and medicinal chemists to initiate programs towards their total synthesis. This paper reviews efforts toward the total synthesis of tubulysins and selected structure-activity relationship studies of tubulysin analogs.
authors.affiliation: School of Pharmacy, Yantai University, Yantai, Shandong, China.
authors.forename: Xu
authors.initials: X
authors.lastname: Xiangming
authors.forename: Gregory K
authors.initials: GK
authors.lastname: Friestad
authors.forename: Yao
authors.initials: Y
authors.lastname: Lei
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000737:chemistry / Q000378:metabolism; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D009842:Oligopeptides; D014404:Tubulin; D050257:Tubulin Modulators