ABSTRACT

Natural product research has made great contributions to drug discovery, with nearly 50% of drugs on the market being natural products or derivatives of natural products.1 Screening crude extracts was common in pre-1980s natural product drug discovery when screening technology was still low throughput. With the advent of high-throughput screening (HTS) in the late 1980s,2 the automated screening of larger sample sets or libraries became possible. The discovery of bioactive natural products involving initial HTS requires the generation of libraries of crude extracts, prepuried fractions, or pure compounds. A screening campaign can be commenced on any of these three libraries as long as the chosen library can deliver the requirements in a fast and cost-effective

CONTENTS

5.1 Introduction ............................................................................................................................ 91 5.2 Lead-Like Enhanced Extract and Fraction Libraries .............................................................92