130064-36-7Relevant academic research and scientific papers
Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity
Chen, Helen Y.,Dykstra, Kevin D.,Birzin, Elizabeth T.,Frisch, Katalin,Chan, Wanda,Yang, Yi T.,Mosley, Ralph T.,DiNinno, Frank,Rohrer, Susan P.,Schaeffer, James M.,Hammond, Milton L.
, p. 1417 - 1421 (2007/10/03)
A class of flavanoids exhibiting a high degree of selectivity for ERα over ERβ has been discovered. The most active analogue 6 was found to be 66-fold ERα-selective and demonstrated uterine estradiol antagonism.
Synthesis and post-coital contraceptive activity of a new series of substituted 2,3-diaryI-2H-1-benzopyrans
Hajela,Kapil
, p. 135 - 142 (2007/10/03)
A series of substituted 2,3-diaryl-2H-1-benzopyrans have been synthesized and screened for their post-coital contraceptive activity in rats. Most of the compounds showed 100% inhibition in a single day schedule at a dose level of 1.0 mg/kg. Compound 32 was found to be the most active with a minimum effective dose (MED) of 0.2 mg/kg in single day testing. Further, it also showed high antiestrogenic activity and is devoid of any agonistic activity.
Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans
-
, (2008/06/13)
A method of inhibiting bone loss comprising administering to an animal an effective amount of a compound having the formula STR1 wherein: R1 and R2 are, independently, --H, --OH, halo, --OC1 -C17 alkyl, --OC3 -C6 cycloalkyl, --O(CO)C1 -C17 alkyl, --O(CO) aryl, --O(CO)O aryl, or --OSO2 -(n-butyl or n-pentyl); R3 is STR2 R4 is --H, methyl, ethyl, propyl, ethenyl or ethynyl; or a pharmaceutically acceptable salt or solvate thereof.
Novel methodology for the synthesis of estrogenic and antiestrogenic isoflav-3-enes
Grese,Grese, Timothy A.,Pennington,Pennington, Lewis D.
, p. 8913 - 8916 (2007/10/02)
A novel and selective method for the introduction of substituents at the 2-position of the isoflav-3-ene nucleus, utilizing readily available 3-arylcoumarins as starting materials, is described. Thus, addition of a Grignard reagent to the corresponding phenyl acetal provided the desired 2-alkyl-, alkenyl-, or arylisoflav-3-enes. These compounds interact strongly with the estrogen receptor and show estrogenic or antiestrogenic effects depending upon the nature of the 2-substituent.
Benzopyrans as antiestrogenic agents
-
, (2008/06/13)
The present invention provides compounds of formula (I) wherein R1 and R2, which may be the same or different, are each -H, -OH, alkoxy of 1 to 17 carbon atoms or alkoxycarbonyl of 2 to 18 carbon atoms and R3 is are useful in the treatment of an estrogen dependent condition such as breast cancer.
Novel benzopyrans and process for their production
-
, (2008/06/13)
The present invention provides compounds of formula I wherein R1 and R2, which may be the same or different, are each -H, -OH, alkoxy of 1 to 17 carbon atoms or alkoxycarbonyl of 2 to 18 carbon atoms and R3 is are useful in the treatment of an estrogen dependent condition such as breast cancer.
Structure-Activity Relationship of Antiestrogens. Phenolic Analogues of 2,3-Diaryl-2H-1-benzopyrans
Sharma, Arun P.,Saeed, Ashraf,Durani, Susheel,Kapil, Randhir S.
, p. 3222 - 3229 (2007/10/02)
Phenolic analogues of 2--3-phenyl-2H-1-benzopyran (1), a novel antiestrogen, were synthesized and evaluated for their structure-activity relationship.Incorporation of OH at position 7 was found to improve receptor affinity of
