Dr. Ryan Murelli
Assistant Professor
Department of Chemistry
Brooklyn College and The Graduate Center, City University of New York
"New Synthetic Methods and Strategies for Drug Discovery and Development"
Abstract: ‘Privileged’ therapeutic pharmacophores offer exciting opportunities for
a broad range of drug development pursuits through a common synthetic
strategy. Our lab has been working on the development of a general and effective
method for the synthesis of 7-hydroxytropolones, which are troponoids that have
been identified as lead drug targets for a variety of diseases from HIV and malaria
to cancer and bipolar disorder. The key step in our strategy is an oxidopyrylium
cycloaddition/ ring-opening sequence, which has proven effective in the synthesis
of a library of new and structurally diverse 7-hydroxytropolones. We are
simultaneously carrying out several medicinal chemistry studies aimed at
optimizing these compounds for potency and selectivity against HIV, Hepatitis B,
Herpes Simplex Virus, drug-resistant bacteria and cancer. Our synthesis and
medicinal chemistry studies thus inspire advancements in each other: Medicinal
chemistry studies inform us of both the advantages and limitations of our chemistry
in its current form and direct new synthetic methods developments, while
discoveries made through our synthetic chemistry studies provides new and
exciting
opportunities
for
drug-development
pursuits.