1-Imidazolyl (alkyl)-substituted di-and tetrahydroquinolines and analogues: Syntheses and evaluation of dual inhibitors of thromboxane A2 synthase and aromatase

C Jacobs, M Frotscher, G Dannhardt…

Index: Jacobs, Christoph; Frotscher, Martin; Dannhardt, Gerd; Hartmann, Rolf W. Journal of Medicinal Chemistry, 2000 , vol. 43, # 9 p. 1841 - 1851

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Citation Number: 61

Abstract

A series of 1-imidazolyl (alkyl)-substituted quinoline, isoquinoline, naphthalene, benzo [b] furan, and benzo [b] thiophene derivatives was synthesized as dual inhibitors of thromboxane A2 synthase (P450 TxA2) and aromatase (P450 arom). Dual inhibition of these enzymes could be a novel strategy for the treatment of mammary tumors and the prophylaxis of metastases. The most potent dual inhibitors, 5-(2-imidazol-1-ylethyl)-7, 8- ...