Novel N-(phosphonomethyl) glycine derivatives: Design, characterization and biological activity.
A series of Calpha,alpha-disubstituted cyclic derivatives of N-(phosphonomethyl) glycine have been synthesized and characterized. They exhibited moderate clastogenicity, low antiproliferative activity on mice bone marrow cells and well expressed cytotoxicity against human tumor cell lines. The 8- and 12-membered cyclic analogs proved superior to the remaining compounds and were found to trigger apoptotic cell death in DOHH-2 cells. The latter compound caused 50% inhibition of the viability of hemobastose-derived cell lines at concentrations ranging from 20 to 67 microM.
Naydenova
Emilia D
ED
University of Chemical Technology and Metallurgy, Department of Organic Chemistry, Sofia 1756, Bulgaria. e_naydenova@abv.bg
Todorov
Petar T
PT
Topashka-Ancheva
Margarita N
MN
Momekov
Georgi Ts
GTs
Yordanova
Tsvetelina Z
TZ
Konstantinov
Spiro M
SM
Troev
Kolio D
KD
D017209:Apoptosis / Q000187:drug effects; D002460:Cell Line; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D009153:Mutagens / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D000097797:Glyphosate
D005998:Glycine; D009153:Mutagens; D000097797:Glyphosate