Synthesis, biological evaluation, structural–activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators

2008 ◽  
Vol 16 (21) ◽  
pp. 9554-9573 ◽  
Author(s):  
Irene Barrett ◽  
Mary J. Meegan ◽  
Rosario B. Hughes ◽  
Miriam Carr ◽  
Andrew J.S. Knox ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Docking Study ◽  
Biological Evaluation ◽  
Activity Relationship ◽  
Estrogen Receptor Modulators ◽  
Structural Activity Relationship ◽  
Receptor Modulators

Synthesis of novel cycloheptylbenzothiazole-2-carboxamides and biological evaluation as human estrogen receptor modulators

2021 ◽  
Vol 1227 ◽  
pp. 129516
Author(s):  
Purushottam Kapse ◽  
Rupesh V. Chikhale ◽  
Mohammad Rizwan Khan ◽  
Saikh M. Wabaidur ◽  
Md Ataul Islam
Keyword(s):  
Estrogen Receptor ◽  
Biological Evaluation ◽  
Estrogen Receptor Modulators ◽  
Human Estrogen Receptor ◽  
Receptor Modulators

scholarly journals Design and Synthesis of Novel Chalcone-Phenylpyranone Derivatives as Estrogen Receptor Modulators

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 30
Author(s):  
Pritam N. Dube ◽  
Yogita B. Thombare ◽  
Vivekanand A. Chatpalliwar
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Docking Study ◽  
Estrogen Receptor Α ◽  
Side Chain ◽  
Design And Synthesis ◽  
Estrogen Receptor Modulators ◽  
Receptor Modulators ◽  
Mcf 7

Selective estrogen receptor modulators (SERMs) are a class of drugs that act on the estrogen receptor (ER). SERMs are used for treatment and reduction of risk of breast cancer. Herewith we had designed, synthesized, and evaluated chalcone-phenylpyran-2-one derivatives bearing a N,N-dimethyl ethylamine side chain for their anti-breast cancer activity on MCF-7 and Zr-75-1 cell lines in-vitro. The pharmacological data indicated that most of tested compounds showed moderate to significant cytotoxicity and high selectivity toward the estrogen receptor. The Structure activity relationaship analyses indicated that compounds 5f with 2,6-dichloro substitution was more effective. Docking study was performed to predict binding orientation towards the estrogen receptor-α.

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