Drug Design and Discovery Program

This program is focused on central activities required for the development of small organic molecules as cancer chemotherapeutic agents. Members of this program use a wide variety of approaches, including chemical, biochemical, cellular, and animal methods to design and discover drugs. These approaches include (but are not limited to):

• Natural Product-Based Drug Design and Discovery
  Synthesis of anti-cancer natural products and analogs thereof. Biological studies on their mechanism of action.
• Biologically-Targeted Drug Design
  Design, synthesis, and biological evaluation of synthetic compounds as potential inhibitors of anti-cancer enzyme targets, and antagonists of anticancer receptors.
• Screening of Biological Targets for Drug Discovery
  Development and utilization of methods, including systems biology methods, for the high-throughput evaluation of potential anticancer agents.
• Preclinical Models for Drug Development
  Evaluation of potential chemotherapeutic and chemopreventative agents in cellular and animal cancer models.

Specific examples of activities in this program include: a) development of new synthetic routes to natural products known to function as antitumor or chemopreventative agents; b) mechanistic evaluation of new anticancer natural products; c) design and synthesis of targeted protein kinase inhibitors; d) design and synthesis of inhibitors of post-translational modifications; e) design and synthesis of topoisomerase inhibitors; f) development of systems methods for discovery of novel potential anti-cancer targets; g) studies of potential chemotherapeutic agents in mouse xenograph and other animal models.