2- and 3-[(Aryl)(azolyl)methyl]indoles as Potential Non-steroidal Aromatase Inhibitors

被引：65

作者：

Lézé, MP

Le Borgne, M

Marchand, P

Loquet, D

Kogler, M

Le Baut, G

Palusczak, A

Hartmann, RW

机构：

[1] Fac Pharm, UPRES EA 1155, Lab Chim Organ & Chim Therapeut, F-44035 Nantes, France

[2] Pharmazeut & Med Chem, D-66041 Saarbrucken, Germany

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2004年 / 19卷 / 06期

关键词：

aromatase; 17-alpha-hydroxylase/17,20-lyase; azoles; breast cancer;

D O I：

10.1080/14756360400004631

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The present study was designed to follow our pharmacomodulation work in the field of non-steroidal aromatase inhibitors. All target compounds 12a-h and 28a-h were tested in vitro for human placental aromatase inhibition, using testosterone or androstenedione as the substrate for the aromatase enzyme and the IC50 and relative potency to aminoglutethimide data are included. A SAR study indicated that 3[(4-fluorophenyl)(1H-imidazol-1-yl)methyl]-1-ethyl-2-methyl-1H-indole (28 g) was a highly potent and selective aromatase inhibitor with IC50 value of 0.025 muM. 28 g was also a weak inhibitor of androstenedione synthesis.

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页码：549 / 557

页数：9

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