Title of article :
Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer Original Research Article
Author/Authors :
Shailesh Kumar، نويسنده , , Shreekant Deshpande، نويسنده , , Vishal Chandra، نويسنده , , Shakti Kitchlu، نويسنده , , Anila Dwivedi، نويسنده , , Vadithe Lakshma Nayak، نويسنده , , Rituraj Konwar، نويسنده , , Yenamandra S. Prabhakar، نويسنده , , Devi Prasad Sahu، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2009
Abstract :
A novel class of 2,3,4-triarylbenzopyrans has been synthesized and were evaluated for their selective estrogen receptor modulation activity and as a therapeutic agent for breast cancer. Among the compounds synthesized, compounds 11a and 12c exhibited 73.91% and 69.24% inhibition as estrogen antagonistic activity, respectively. Compound 12a showed the lowest IC50 at 6.97 μM against MCF-7 and 11f showed the lowest IC50 value of 5.6 μM against MDA-MB-231 cell line in spite of their low receptor binding affinity implicating these compounds probably act through ER independent mechanism.
Keywords :
2?-Deoxy-5-fluorouridine (5-FdU) , 3?-C-Ethynylcytidine (ECyd) , Hydrogenphosphonate method , Cytostatic duplex drugs , Antimetabolites
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry