Natural product-based drug discovery

Natural products (NPs) represent a unique and highly prolific source of drugs and lead structures for new drug discovery. A significant fraction of the drugs that form the foundations of modern pharmacotherapy are derived from a NP, either directly or indirectly. At the same, time the drug discovery potential of NPs is far from exhausted. For example, it has been estimated that only ca. 6% of higher plants have been systematically investigated pharmacologically (and only some 15% phytochemically); as for the marine environment as source of novel drug leads, this remains virtually unexplored to date. In addition, recent advances in the areas of combinatorial biosynthesis, mutasynthesis and the activation of silent gene clusters in bacteria provide for a further extension of NP structural diversity. Total synthesis has an important role to play in the continuing exploitation of NPs as leads for drug discovery.[Continued at Total Synthesis of Bioactive Natural Products]. Last but not least, it should be highlighted that the 2015 Nobel Prize in Physiology or Medicine was awarded for the development of natural products into drugs against diseases afflicting millions of people worldwide, i. e. ivermectin and artemisinin. The Prize was divided, one half jointly to William C. Campbell and Satoshi Ōmura "for their discoveries concerning a novel therapy against infections caused by roundworm parasites" (ivermectin) and the other half to Youyou Tu "for her discoveries concerning a novel therapy against Malaria" (artemisinin).

Additional reading:

K.-H. Altmann. Drugs from the oceans: marine natural products as leads for drug discovery. Chimia 2017, 71, 646-652. external pagehttps://doi.org/10.2533/chimia.2017.646call_made

E. Patridge, P. Gareiss, M. S. Kinch, D. Hoyer. An analysis of FDA-​approved drugs: natural products and their derivatives. Drug Discov. Today 2016, 21, 204-207. external pagehttps://doi.org/10.1016/j.drudis.2015.01.009call_made

G. M. Cragg, D. J. Newman. Natural Products As Sources of New Drugs from 1981 to 2014. J. Nat. Prod. 2016, 79, 629-661. external pagehttp://pubs.acs.org/doi/abs/10.1021/acs.jnatprod.5b01055call_made

D. Camp, A. Garavelas, M. Campitelli. Analysis of Physicochemical Properties for Drugs of Natural Origin. J. Nat. Prod. 2015, 78, 1370-1382. external pagehttp://pubs.acs.org/doi/abs/10.1021/acs.jnatprod.5b00255call_made

G. M. Cragg, Paul G. Grothaus, D. J. Newman. New Horizons for Old Drugs and Drug Leads. J. Nat. Prod. 2014, 77, 703-723. external pagehttp://pubs.acs.org/doi/pdf/10.1021/np5000796call_made

Nobel Lecture, Youyou Tu: external pagehttps://www.nobelprize.org/prizes/medicine/2015/tu/lecture/call_made

Nobel Lecture, William C. Campbell: external pagehttps://www.nobelprize.org/prizes/medicine/2015/campbell/lecture/call_made

Nobel Lecture, Satoshi Õmura: external pagehttps://www.nobelprize.org/prizes/medicine/2015/omura/lecture/call_made