title: Cytotoxic simplified tubulysin analogues.
abstract: An efficient route for the synthesis of the tubulysin family of antimitotic peptides was developed. Simplified tubulysin analogues were synthesized to define the minimum pharmacophore required for cytotoxicity. Simplified tubulysin analogues retain significant cytotoxicity and reveal important preliminary structure-activity relationships.
authors.affiliation: Department of Medicinal Chemistry. 308 Harvard Street SE, University of Minnesota, Minneapolis, MN 55455, USA.
authors.forename: Bhooma
authors.initials: B
authors.lastname: Raghavan
authors.forename: Ranganathan
authors.initials: R
authors.lastname: Balasubramanian
authors.forename: Jaeson C
authors.initials: JC
authors.lastname: Steele
authors.forename: Dan L
authors.initials: DL
authors.lastname: Sackett
authors.forename: Robert A
authors.initials: RA
authors.lastname: Fecik
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008968:Molecular Conformation; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013997:Time Factors
chemical_list: D000970:Antineoplastic Agents; D009842:Oligopeptides; C510756:tubulysin A; C502386:tubulysin D