Chemotherapy Treatment: SN-38 Bifunctional Small Molecules for Localized Estrogen Receptor Targeting

September 17, 2024 Colloquia Presenters

Department of Chemistry, Biochemistry & Physics

Development of SN-38 Bifunctional Small Molecules for Localized Estrogen Receptor Targeting As Selective Chemotherapy Treatment

Targeted therapeutic treatments in chemotherapy have made recent advancements in antibody drug conjugates, but those compounds face issues in scalability. A recent report from the Crews lab demonstrated significant efficacy in a novel small molecule targeting system called RIPTACs. By linking an inhibitor drug with a targeting ligand, this bifunctional molecule would selectively target cancerous cells. Current efforts are working toward linking the ER-targeting ligands estradiol and tamoxifen with the topoisomerase I inhibitor SN-38. Estradiol and tamoxifen act as traditional ER-positive breast cancer treatments through active inhibition of estrogen. We aim to establish a synthetic pathway for effectively linking the two drugs and to assay the compounds in breast and colon cancer cell lines to determine their biological activity.

RESEARCHERS: Isabella L., The Harker School '25, Terry W., Mission San Jose High School' 25

ADVISOR: Njoo Synthesis | Physical Organic Chemistry | Catalysis | Chemical Biology | Spectroscopy | Medicinal Chemistry

KEYWORDS: Natural Products | Tubulin Inhibitors | Chemical Biology