Synthesis and antiproliferative activity of aromatic and aliphatic bis[aminomethylidene(bisphosphonic)] acids.
A series of aromatic and aliphatic bis[aminomethylidene(bisphosphonic)] acids was synthesized in the reaction of triethylphosphite with isonitriles followed by hydrolysis or dealkylation. The in vitro anti-proliferative effect of all synthesized tetraphosphonic acids against MCF-7 breast cancer cells, J774E macrophages and HL-60 promyelocytic leukemia cells was determined. Three aromatic derivatives (5a, 5f and 5j) showed a similar or higher anti-proliferative activity than zoledronic acid.
['Goldeman|Waldemar|W|', 'Nasulewicz-Goldeman|Anna|A|']
D015057:1-Naphthylamine D000814:Aniline Compounds D000970:Antineoplastic Agents D045744:Cell Line, Tumor D049109:Cell Proliferation D004164:Diphosphonates D004305:Dose-Response Relationship, Drug D004354:Drug Screening Assays, Antitumor D018922:HL-60 Cells D006801:Humans D061986:MCF-7 Cells D008264:Macrophages D015394:Molecular Structure D010655:Phenylenediamines D013329:Structure-Activity Relationship
Isonitrile Tetraphosphonate Anti-proliferative activity Bisphosphonate Bisphosphonic acid Isocyanide Osteoclasts Tumor cells