Tyrenes: synthesis of new antiproliferative compounds with an extended conjugation.
A series of substituted styryl-acrylonitriles was designed and synthesized. The new compounds, called tyrenes, were tested for the ability to inhibit acute lymphocytic leukemia (ALL) cancer cell growth, as well as on their toxicity to normal bone marrow (NBM) cells. The results showed that 3,4-dihydroxystyryl-acrylonitriles, in particular CR-4, revealed great potency as antitumor agents, and also exhibited low toxicity to normal cells. The effectiveness of these compounds with extended conjugation may be due to their possible functioning as reactive Michael acceptors.
Demin
Peter
P
Division of Immunology and Allergy, Infection, Immunity, Injury and Repair Program, Research Institute, and The Hospital for Sick Children and University of Toronto, Toronto, Canada M5G 1X8.
Rounova
Olga
O
Grunberger
Thomas
T
Cimpean
Lorand
L
Sharfe
Nigel
N
Roifman
Chaim M
CM
D000181:Acrylonitrile / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D013343:Styrenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D013343:Styrenes; D000181:Acrylonitrile