Organic phenyl arsonic acid compounds with potent antileukemic activity.

A series of 12 organic arsonic acid compounds has been synthesized and evaluated against human B-lineage (NALM-6) and T-lineage (MOLT-3) acute lymphoblastic leukemia (ALL) cell lines. The lead compounds 2-trichloromethyl-4-[4′-(4″-phenylazo)phenylarsonic acid]aminoquinazoline (compound 19, PHI-P518; IC50=1.1±0.5 μM against NALM-6 and 2.0±0.8 μM against MOLT-3) and 2-methylthio-4-(2′-phenylarsonic acid)aminopyrimidine (compound 15, PHI-P381; IC50=1.5±0.3 μM against NALM-6 and 2.3±0.5 μM against MOLT-3) exhibited potent antileukemic activity at low micromolar concentrations.