Michael McParlan

There is estimated be 1.8 million new cancer cases in the United States by the completion of 2020, showing the need for new therapies. Introduction of new therapies has proven to take extensive time and money to be approved for clinical use. To expedite this process clinically approved drugs with anticancer effects can be used as templates to improve upon their pharmacokinetic, pharmacodynamic, and cytotoxic abilities. Telmisartan, an antihypertensive agent, has shown activity toward different forms of cancer, including triple negative breast cancer. However, structure activity relationships have shown the polar carboxylic acid moiety is integral for inhibiting the renin-angiotensin-aldosterone system and potentially reduces solubility. Coupling of the acid to various amide derivative gives potential to improve membrane permeability and improve upon the anticancer effects while removing the antihypertensive effects of Telmisartan. In this regard 14 derivatives were synthesized and screened against 4T1, WiDr, MDA-231, MIAPaCa-2 and MCF-7 cancer cell lines. Via the MTT colorimetric assay these derivatives have shown to have low micromolar potency, over ~10 times the potency of Telmisartan.