Biomedical Engineering Reference
In-Depth Information
15
CHAPTER
TARGET-ORIENTED
AND DIVERSITY-ORIENTED
ORGANIC SYNTHESIS
RAPHA
¨
L RODRIGUEZ
Department of Chemistry, Cambridge University, Cambridge, United Kingdom
It is not because things are difficult that we do not dare;
it is because we do not dare that they are difficult
—Seneca (4 BC-65 AD)
15.1.
INTRODUCTION
Natural products and synthetic small molecules are central players in chemical
biology studies [1]. They promote the perturbation of cellular processes underlying
diseases and facilitate the discovery of biological targets that can be validated for
therapeutic intervention. Small molecules have been shown to accurately tune a single
function of pluripotent proteins in a reversible and dose-dependant manner with
temporal resolution that is hardly achievable by current molecular biology methods.
Hence, small molecule approaches are complementary to RNA interference strategies
and offer the additional means of identifying an associated chemical hit suitable for
drug development. The efficient synthesis of molecular probes and drugs remains a
worthy challenge that can be addressed by the invention of novel high-yielding and
stereoselective synthetic methods.
15.2. TARGET-ORIENTED AND DIVERSITY-ORIENTED
SYNTHESIS
Over the past two centuries, synthetic organic chemistry has undergone a remarkable
development. Total synthesis began with the preparation of urea in 1828 [2].
Scientists finally reproduced Nature's accomplishment and accumulated enough
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