NOVEL NONCROSS-RESISTANT DIAMINOANTHRAQUINONES AS POTENTIAL CHEMOTHERAPEUTIC-AGENTS

被引：12

作者：

JIANG, JB

JOHNSON, MG

DEFAUW, JM

BEINE, TM

BALLAS, LM

JANZEN, WP

LOOMIS, CR

SELDIN, J

COFIELD, D

ADAMS, L

CIANCIOLO, G

DEGEN, D

VONHOFF, DD

机构：

[1] SPHINX PHARMACEUT CORP, DEPT BIOCHEM RES, DURHAM, NC 27717 USA

[2] SPHINX PHARMACEUT CORP, DEPT PRECLIN DEV, DURHAM, NC 27717 USA

[3] UNIV TEXAS, HLTH SCI CTR, SAN ANTONIO, TX 78284 USA

[4] CANC THERAPY & RES CTR, SAN ANTONIO, TX 78284 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 23期

关键词：

D O I：

10.1021/jm00101a001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of diaminoanthraquinones was discovered initially as protein kinase C inhibitors with IC50s in the 50-100 muM 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.

引用

页码：4259 / 4263

页数：5

共 15 条

[1]

Bell R M, 1986, Methods Enzymol, V124, P353

[2]

DUMONT JA, 1992, CANCER RES, V52, P1195

[3]

GRUNICKE H, 1989, ADV ENZYME REGUL, V28, P201

[4] TUMOR-CELL ADHERENCE TO CULTURED CAPILLARY ENDOTHELIAL-CELLS IS PROMOTED BY ACTIVATORS OF PROTEIN-KINASE-C [J].