[Synthesis of thiophene and alpha-terthiophene derivatives with antiproliferative activity].
We have synthesised a series of known alpha-terthiophene lead molecules with PKC (protein kinase C) inhibitory activity and the compounds were tested in cell proliferation assay on EGF-RTK (epidermal growth factor receptor protein tyrosine kinase) over-expressing tumour cell line (A431). We found that two of them had excellent antiproliferative activity. We prepared a focused molecule library around the thiophene and the terthiophene scaffold and examined these compounds in cell proliferation assay on A431.
Székelyhidi
Zsolt
Z
Semmelweis Egyetem, Kooperációs Kutató Központ, Budapest.
Pató
János
J
Hegymegi-Barakonyi
Bálint
B
Bánhegyi
Péter
P
Mészáros
György
G
Kéri
György
G
Orfi
Lászlo
L
D000890:Anti-Infective Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000494:pharmacology; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D006801:Humans; D011493:Protein Kinase C / Q000037:antagonists & inhibitors; D013876:Thiophenes / Q000494:pharmacology*
D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D013876:Thiophenes; C019101:alpha-terthienyl; D066246:ErbB Receptors; D011493:Protein Kinase C