Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer.
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 IC(50) at 6.97 microM against MCF-7 and 11f showed the lowest IC(50) value of 5.6 microM against MDA-MB-231 cell line in spite of their low receptor binding affinity implicating these compounds probably act through ER independent mechanism.
Kumar
Shailesh
S
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
Deshpande
Shreekant
S
Chandra
Vishal
V
Kitchlu
Shakti
S
Dwivedi
Anila
A
Nayak
Vadithe Lakshma
VL
Konwar
Rituraj
R
Prabhakar
Yenamandra S
YS
Sahu
Devi Prasad
DP
D001578:Benzopyrans / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004965:Estrogen Antagonists; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D011960:Receptors, Estrogen / Q000378:metabolism; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis*
D001578:Benzopyrans; D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators