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14th World Congress on Chemistry

Barcelona, Spain

Shaymaa E. Kassab

Associate Professor of Medicinal Chemistry

Title: Structure-based design and synthesis of conformationally constrained derivatives of methyl-piperidinopyrazole (MPP) with estrogen receptor (ER) antagonist activity

Biography

Biography: Shaymaa E. Kassab

Abstract

 

Nuclear Estrogen Receptors (ER) is cytoplasmic proteins; translocated to the nucleus to induce transcriptional signals after getting bound to the estrogen hormone. ER activation implicated in cancer cell proliferation of female reproductive organs. Thus, the discovery of ER antagonists is a reliable strategy to combat estrogen dependent breast cancer. Endometrial carcinoma is one of the complications encountered upon long-term therapy by Selective Estrogen Receptor Modulators (SERMs) like Tamoxifen (TMX) and Methyl Piperidino Pyrazole (MPP). Thus, the ER-full antagonist is a solution to improve the safety of this class of therapeutics during the treatment of breast cancer.