Design and synthesis of a fluoroindolocarbazole series as selective topoisomerase I active agents.: Discovery of water-soluble 3,9-difluoro-12,13-dihydro-13-[6-amino-β-D-glucopyranosyl]-5H,13H-benzo[b]-thienyl[2,3-α]pyrrolo[3,4-c]carbazole-5,7(6H)-dione (BMS-251873) with curative antitumor activity against prostate carcinoma xenograft tumor model

被引：30

作者：

Balasubramanian, BN

Laurent, DRS

Saulnier, MG

Long, BH

Bachand, C

Beaulieu, F

Clarke, W

Deshpande, M

Eummer, J

Fairchild, CR

Frennesson, DB

Kramer, R

Lee, FY

Mahler, M

Martel, A

Naidu, BN

Rose, WC

Russell, J

Ruediger, E

Solomon, C

Stoffan, KM

Wong, H

Zimmermann, K

Vyas, DM

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

[2] Candiac, Montreal, PQ, Canada

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 07期

关键词：

D O I：

10.1021/jm034197s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of fluoroindolocarbazoles were studied with respect to their topoisomerase I activity, cytotoxicity, selectivity, and in vivo antitumor activity. Emerging from this series was BMS-251873, a potential clinical candidate possessing a robust pharmacological profile including curative antitumor activity against prostate carcinoma.

引用

页码：1609 / 1612

页数：4

共 15 条

[1] OXYGEN HETEROCYCLES .3. THE REACTIVITY OF BENZOFURAN AND 2-ALKYLBENZOFURANS [J].