Tetrahydroquinoline‐Based Selective Estrogen Receptor Modulators (SERMs).

Abstract

Quinoline derivatives Quinoline derivatives R 0410Tetrahydroquinoline-Based Selective Estrogen Receptor Modulators (SERMs).-The design and synthesis of a series of substituted tetrahydroquinolines such as (VI) and (X) starting from commercially available N-oxide (I), their binding affinities to estrogen receptors and antagonism of estradiol in MCF-7 breast adenocarcinoma cells are reported. Compound (X) is the most potent inhibitor of MCF-7 proliferation identified in this series. -(WALLACE*, O. B.; LAUWERS, K. S.; JONES, S. A.; DODGE, J. A.; Bioorg. Med.

Estrogen receptor β ligands: Recent advances and biomedical applications

“…Consequently, the selectivity ratio was also reduced, dropping to 2.6 for 89, while 84 showed an almost 10-fold selectivity for ERb over ERa. 96 Pfizer has described the preparation of several 1,2,3,4-tetrahydroisoquinolines, among which some ERb-selective ligands were found. 97 This is the case for compounds 90 and 91 ( Fig.…”

Synthesis and Antimicrobial Activity of Some Novel N-Mannich Bases of Imidazole Phenylazetidin-2-one

“…The synthesis of β-lactam antibiotics has occupied an important place in the field of medicinal and research pharmaceutical. The antibiotic activity of Azetidine-2-ones (β-lactam) possessing antiviral, antifungal activities, antithrombotic and cholesterol inhibition [1][2][3][4].…”

Synthesis and X-ray powder diffraction data of cis-4-(4-methoxyphenyl)-3-methyl-6-nitro-2-phenyl-1,2,3,4-tetrahydroquinoline

“…Many pharmaceutical agents and different natural products with significant biological activity are built on the (tetrahydro)quinoline scaffolds (Katritzky et al , 1996; Kouznetsov et al , 1998). A large number of reports showed that these compounds display a wide spectrum of biological activities, including antimalarial activity (Bendale et al , 2007), estrogenic receptor (Wallace et al , 2003; Chen, et al , 2007), anti-inflammatory behavior (Calhoun et al 1995), among others.…”