Design, synthesis, and biological evaluation of levoglucosenone-derived ras activation inhibitors.
A panel of new potential Ras ligands was generated by decorating a tricyclic levoglucosenone-derived scaffold with aromatic moieties. Some members of the panel show in vitro inhibitory activity toward the nucleotide exchange process on Ras and are toxic to some human cancer cell lines.
Müller
Christian
C
B. U. Oncology, Nerviano Medical Sciences, MI, Italy.
Gomez-Zurita Frau
Maria Antonia
MA
Ballinari
Dario
D
Colombo
Sonia
S
Bitto
Alessandro
A
Martegani
Enzo
E
Airoldi
Cristina
C
van Neuren
Anske Stephanie
AS
Stein
Matthias
M
Weiser
Jörg
J
Battistini
Carlo
C
Peri
Francesco
F
D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005947:Glucose / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D018631:ras Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism
D019086:Bridged Bicyclo Compounds, Heterocyclic; D004791:Enzyme Inhibitors; C512757:1,6-anhydro-3,4-dideoxyhex-3-enopyran-2-ulose; D018631:ras Proteins; D005947:Glucose