Novel non-cross resistant diaminoanthraquinones as potential chemotherapeutic agents.
A novel series of diaminoanthraquinones was discovered initially as protein kinase C inhibitors with IC50s in the 50-100 microM range. They exhibited potent tumor cell growth inhibitory activity in vitro without cross resistance to adriamycin. Further evaluation of two of the most active compounds NSC 639365 (3) and NSC 639366 (4) in human tumor cloning assay showed potent cytocidal activity. The results suggest therapeutical potentials against human tumors.
Jiang
J B
JB
Department of Chemical Research, Sphinx Pharmaceuticals Corporation, Durham, North Carolina 27717.
Johnson
M G
MG
Defauw
J M
JM
Beine
T M
TM
Ballas
L M
LM
Janzen
W P
WP
Loomis
C R
CR
Seldin
J
J
Cofield
D
D
Adams
L
L
D000880:Anthraquinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002455:Cell Division / Q000187:drug effects; D006801:Humans; D011493:Protein Kinase C / Q000037:antagonists & inhibitors; D014407:Tumor Cells, Cultured / Q000187:drug effects; D014410:Tumor Stem Cell Assay
D000880:Anthraquinones; D000970:Antineoplastic Agents; D011493:Protein Kinase C