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; IC(50)=1.1+/-0.5 microM against NALM-6 and 2.0+/-0.8 microM against MOLT-3) and 2-methylthio-4-(2'-phenylarsonic acid)aminopyrimidine (compound 15, PHI-P381; IC(50)=1.5+/-0.3 microM against NALM-6 and 2.3+/-0.5 microM against MOLT-3) exhibited potent antileukemic activity at low micromolar concentrations.
Liu
Xing-Ping
XP
Parker Hughes Cancer Center, Parker Hughes Institute, 2699 Patton Road, St. Paul, MN 55113, USA.
Narla
Rama Krishna
RK
Uckun
Fatih M
FM
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001152:Arsenicals / Q000138:chemical synthesis* / Q000494:pharmacology*; D019070:Cell Lineage; D016158:Genes, p53 / Q000235:genetics; D006801:Humans; D007938:Leukemia / Q000188:drug therapy*; D054198:Precursor Cell Lymphoblastic Leukemia-Lymphoma / Q000188:drug therapy; D013778:Tetrazolium Salts / Q000737:chemistry; D013844:Thiazoles / Q000737:chemistry; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D001152:Arsenicals; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue