Cytotoxic simplified tubulysin analogues.
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.
Raghavan
Bhooma
B
Department of Medicinal Chemistry. 308 Harvard Street SE, University of Minnesota, Minneapolis, MN 55455, USA.
Balasubramanian
Ranganathan
R
Steele
Jaeson C
JC
Sackett
Dan L
DL
Fecik
Robert A
RA
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
D000970:Antineoplastic Agents; D009842:Oligopeptides; C510756:tubulysin A; C502386:tubulysin D