Natural product drug development

Substituted 1,3-diols are valuable intermediates in the synthesis of drugs and natural products [18]. Starting from the regio- and enantioselective enzymatic reduction of diketo esters described above, various methods to obtain enantio-merically pure 3,5-dihydroxy esters were developed. 

We have shown organocatalysis to be a powerful tool for the synthesis of drugs and natural products. Our work and that of others have clearly demonstrated that organocatalytic strategies can cut down the total number of synthetic operations. As organocatalysts are usually non-toxic, air- and moisture-stable and often available from renewable sources, they are destined to have an impact on the development of future sustainable chemical processes. 

Subsequently, solid-phase strategies were developed for the synthesis of oligonucleotides, as well as for nonbiopolymer small molecules, such as synthetic drugs and natural products. In a solid-phase synthesis, the starting material (e.g., first residue or molecular scaffold) is attached to an insoluble solid support, such as a polymer or glass bead, via a chemical linker that can be cleaved under specific, orthogonal reaction conditions... 

M. Sufihess, "The Discovery and Development of Antitumor Drugs from Natural Products" in "Advances in Medicinal Plant Research", ed by A. J. Vlietinck and R. A. Dommisse, pp. 101 - 133 (1985), Wissenschat liche Verlagsgeselschaft mbH, Stuttgart. 

Commercial evidence also supports the case for natural products. Of the 20 best-selling non-protein drugs in 1999, nine were either derived from or developed as the result of leads generated by natural products (e.g., simvastatin, lovastatin, ciprofloxacin, clarithromycin and cyclosprin) with combined annual sales of greater than US 16 billion. Newer developments based on natural products include the antimalarial drug artemisinin, and the anticancer agents taxol, docetaxel and camptothecin. In addition to the historical success in drug discovery, natural products are likely to continue to be sources of new commercially viable... 

Quinn, R.J., Carroll, A.R., Pham, NJ5., Baron, P., Palftaman, M.E., Suraweera, L., Pierens, G.K., and Muresan, S. (2008) Developing a drug-like natural product library. Journal of Natural Products, 71, 464-468. 

N. Ikekawa, in H. Danielsson and. Sjovah, eds.. Steroids andBile Acids, Elsevier Science Pubhshers BV, Amsterdam, the Nethedands, 1985, pp. 199—230 C. Djerassi, in P. Krogsgaard-Larsen, S. Brogger Christensen, and H. Kofod, eds., Alfred Benpon Symposium 20 Natural Products and Drug Development, Munksgaard, Copenhagen, Denmark, 1984, pp. 164—176 N. W. Withers, in P. J. Scheuer, ed.. Marine Natural Products, Vol. V, Academic Press, Inc., New York, 1983, pp. 87—130 C. Djerassi, Pure Appl Chem. 53, 873 (1981). 

A. Aituso, Drugs of Natural Origin Economic and Policy Aspects of Discovery, Development, and Marketing, The Pharmaceutical Products Press, New York, 1997, p. 142. 

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