Estrogen receptor, aromatase and 17-ßHSD inhibitors are main target of pharmacological interest for the treatment of estrogen dependent cancers.Proposed ligands having estrogen receptor domains and this rationale has led to work on the development of “multiple targets” class of drugs that would modulate the action of estrogens and thereby interfere with, or even prevent, the proliferation of breast and uterine cancer cells. 4-methoxy Tamoxifen was taken as standard which has shown affinity toward estrogen receptors. Thus, the PDB ID: 1QKU and 3ERT binding site is potentially a good target for new anticancer drugs that will directly inhibit metastasis. Docking studies using the structure of the 1QKU binding domain suggested that 3-methyl-2-phenyl-2,3-dihydrochromen-4-one derivatives substituted at position C-5 and C-6 could be good candidates. Series of flavone derivatives were synthesized and evaluated by Preliminary in-vitro cytotoxicity was checked by sulphorhodamine B assay and for promising molecule, five dose assay in prostate cancer cell line PC-3, ER negative cell line (MDA-MB 453) and determination of IC50 by SRB assay. In addition, mechanistic study was done with cytometric analysis and electrophoretic determination of apoptosis. For In-vivo activity, evaluation of anti-tumor activity of selected synthetic compounds by Ehrlich Ascites Carcinoma (EAC) model and related studies was performed.

Phytoestrogens: New ligands targeting the estrogen receptor domains

253rd National Meeting (2017)

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