139276-11-2Relevant articles and documents
Benzofurans used to inhibit bone loss
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, (2008/06/13)
The present invention provides methods for inhibiting bone loss comprising administering to a mammal in need of treatment of a bone loss inhibiting amount of a compound of formula I STR1 wherein R is hydrogen or methyl; R1 and R2 each are methyl or ethyl, or R1 and R2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group; and X is bromo, chloro, fluoro, or hydrogen; or a pharmaceutically acceptable salt thereof.
Benzofuran derivatives for inhibiting uterine fibroid disease
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, (2008/06/13)
The present invention provides a method for inhibiting uterine fibroid disease comprising administering to a woman in need of treatment an effective amount of a compound of formula I wherein, ???R is hydrogen or methyl;, ???R1and R2each are methyl or ethy, or R1and R2together with the nitrogen atom to which they are attached represent a saturated heterocyclic group; and, ???X is bromo, chloro, fluoro, or hydrogen; or a pharmaceutically acceptable salt thereof.
Synthesis of 2-(p-Chlorobenzyl)-3-aryl-6-methoxybenzofurans as Selective Ligands for Antiestrogen-Binding Sites. Effects on Cell Proliferation and Choresterol Synthesis
Teo, Chin Chin,Kon, Oi Lian,Sim, Keng Yeow,Ng, Siu Choon
, p. 1330 - 1339 (2007/10/02)
A series of nonsteroidal compounds, 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans derived from the 2-(p-chlorobenzyl)-6-methoxy-3(2H)-benzofuranones has been synthesized.The key steps in the synthesis were reactions of 2-(p-chlorobenzyl)-6-methoxy-3(2H)-benzofuranones with the arylorganometallic reagents followed by dehydration of the resulting carbinols.The benzofurans are ligands for antiestrogen-binding sites (AEBS) and display no significant interaction with the estrogen receptor (ER).All bind to AEBS with equivalent or greater affinity than tamoxifen.These compounds decrease thymidine incorporation in AEBS-containing EL4 lymphoid cells and MCF7 breast cancer cells in a concentration-dependent manner between 10-8 and 10-6 M and are generally more inhibitory than tamoxifen.In contrast, they have no effect on thymidine incorporation by an AEBS-deficient variant of the MCF7 cell line, RTx6.The present findings of (1) selective and high affinity binding of the benzofurans to AEBS, (2) their concentration-dependent inhibition of thymidine incorporation in AEBS-containing cells, and (3) their lack of antiproliferative effect in an AEBS-deficient cell line suggest a functional role for AEBS in mediating the antigrowth effect of these compounds.Two of the more active benzofuran compounds also significantly inhibited de novo cholesterol biosynthesis in EL4 cells which lack ER.This effect could be obtained after 5 h of treatment and preceded significant loss of cell viability.This is the first demonstration that selective ligands of AEBS (other than the known nonsteroidal antiestrogens) interfere with cholesterol biosynthesis - an action that may contribute to their antigrowth effect.
