Diversity-Oriented Synthesis and Rational Drug Design for Chemical Biology and Drug Discovery Research

Research in the Tan Lab focuses on synthetic organic chemistry and its applications to current challenges in chemical biology and drug discovery.

Rational Drug Design of Adenylation Enzyme Inhibitors

Adenylation enzymes mediate a variety of important bacterial and eukaryotic pathways. We are using rational drug design to develop sulfonyladenosine-based inhibitors of adenylation enzymes as new antibiotics and chemical probes.

Stereoselective Diversity-Oriented Synthesis of Spiroketals

Spiroketals are privileged substructures found in numerous natural products with diverse biological activities. We are developing stereoselective diversity-oriented synthesis routes to provide spiroketal libraries with comprehensive stereochemical diversity for screening against a wide range of biological targets.

Diversity-Oriented Synthesis of Polyketides

Polyketides exhibit an impressive range of biological activities, with examples from the anticancer arena including discodermolide, depudecin, and trichostatin. We are developing versatile diversity-oriented synthesis routes that provide polyketide fragments having both stereochemical and skeletal diversity.

Diversity-Oriented Synthesis of Multiscaffold Polycyclic Libraries

An amazing range of rigid, densely functionalized polycyclic compounds are formed from simple precursors during the biosynthesis of alkaloids and terpenoids. To access such structures, we are using a related diversity-oriented synthesis strategy to generate multiscaffold polycyclic libraries from a small set of simple precursors.

Diversity-Oriented Synthesis of Macrocycles

Macrocycles are an attractive class of molecules for use in biological screening. While smaller molecules have been used to bind in enzyme active sites and other protein pockets, larger molecules such as macrocycles may be useful for affecting protein-protein interactions involving large surface areas… .