title: Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer.
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 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.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
authors.forename: Shailesh
authors.initials: S
authors.lastname: Kumar
authors.forename: Shreekant
authors.initials: S
authors.lastname: Deshpande
authors.forename: Vishal
authors.initials: V
authors.lastname: Chandra
authors.forename: Shakti
authors.initials: S
authors.lastname: Kitchlu
authors.forename: Anila
authors.initials: A
authors.lastname: Dwivedi
authors.forename: Vadithe Lakshma
authors.initials: VL
authors.lastname: Nayak
authors.forename: Rituraj
authors.initials: R
authors.lastname: Konwar
authors.forename: Yenamandra S
authors.initials: YS
authors.lastname: Prabhakar
authors.forename: Devi Prasad
authors.initials: DP
authors.lastname: Sahu
mesh_terms: 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*
chemical_list: D001578:Benzopyrans; D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators