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Research Summary

Nicolaou’s research focuses on the advancement of organic synthesis for its own sake and its application to the synthesis of natural and designed molecules of biological and medical importance. Past accomplishments include the total syntheses of the naturally occurring antibiotics amphotericin B, vancomycin and viridicatumtoxin and their analogues, the anticancer agents Taxol®, calicheamicin γ1I, and rapamycin and their analogues, the marine neurotoxins brevetoxins A and B and the azaspiracids, and large segments of maitotoxin, the largest secondary metabolite and most potent nonproteinoic neurotoxin known to date. His research has also led to the structural revisions of numerous natural products and the discovery and development of many synthetic strategies and technologies.

Current projects in the group include the total synthesis of highly potent and scarce naturally occurring cytotoxic molecules and their analogues as payloads for antibody-drug conjugates (ADCs) for targeted personalized cancer therapies. These include the rare natural products shishijimicins, trioxacarcins, tubulysins, thailanstatins, epothilones, uncialamycins, disorazoles and namenamicins.



K.C. Nicolaou was born on July 5, 1946 in Cyprus, where he attended school until the age of 18. In 1964, he emigrated from Cyprus to England where he spent two years learning English and preparing to enter the university. His advanced studies in chemistry were carried out at the University of London (B.Sc., 1969, Bedford College, First Class Honors; Ph.D. 1972, University College, with Profs. F. Sondheimer and P.J. Garratt). In 1972, he crossed the Atlantic to the United States and completed postdoctoral appointments at Columbia University (1972–1973, Prof. T.J. Katz) and Harvard University (1973–1976, Prof. E.J. Corey) after which he joined the faculty at the University of Pennsylvania, where he rose through the ranks to become the Rhodes-Thompson Professor of Chemistry. In 1989, he accepted joint appointments at the University of California, San Diego, where he was Distinguished Professor of Chemistry, and The Scripps Research Institute, where he served as the Chairman of the Department of Chemistry and held the Darlene Shiley Chair in Chemistry and the Aline W. and L. S. Skaggs Professorship of Chemical Biology (1996–2013) in the Department of Chemistry. From 2003 to 2009, he concurrently served as the Founder and Director of the Chemical Synthesis Laboratory at A*STAR, Biopolis in Singapore.  From 2012-2014, he was Visiting Professor at Chongqing University, China. In May 2013, Dr. Nicolaou joined Rice University as the Harry C. and Olga K. Wiess Professor of Chemistry in the BioScience Research Collaborative.

For his scientific work, Professor Nicolaou has received numerous awards and honors, including the Humboldt Foundation US Senior Scientist Prize (Germany, 1987), the A.C. Cope Scholar Award, American Chemical Society (1987), the Award for Creative Work in Synthetic Organic Chemistry, American Chemical Society (1993), the Dr. Paul Janssen Prize for Creativity in Organic Synthesis, Janssen Research Foundation (1994), the Rhone-Poulenc Medal, Royal Society of Chemistry (U.K., 1995), the William H. Nichols Medal, New York Section-American Chemical Society (1996), the Inhoffen Medal, Gesellschaft fur Biotechnologische Forschung mbH (GBF) (Germany, 1996), the Ernest Guenther Award in the Chemistry of Natural Products, American Chemical Society (1996), the Chemical Pioneer Award, American Institute of Chemists (1996), the Linus Pauling Medal, Oregon, Portland, Puget Sound Sections-American Chemical Society (1996), the Decoration of the Order of the Commander of Honor Medal (bestowed by the President of Greece, 1998), the Gustavus John Esselen Award for Chemistry in the Public Interest, Northeastern Section-American Chemical Society (1998), the Yamada Prize (Japan, 1999), the first Aspirin Prize for Solidarity through Chemistry (Spain, 1999), the Max Tishler Lecture Prize, Harvard University (2000), the Paul Karrer Gold Medal, Universität Zürich (Switzerland, 2000), the Centenary Medal, Royal Society of Chemistry (U.K., 2000–2001), the Ernst Schering Prize, Ernst Schering Research Foundation (Germany, 2001), the Nagoya Gold Medal of Organic Chemistry, Nagoya University (Japan, 2001), Tetrahedron Prize for Creativity in Organic Chemistry (2002), the ACS Nobel Laureate Signature Award for Graduate Education in Chemistry (2003), the Aristeio Bodossaki Prize (Greece, 2004), the A.C. Cope Award, American Chemical Society (2005), Auburn-G. M. Kosolapoff Award, Auburn Section-American Chemical Society (2006), the Burkardt-Helferich Prize (2006), the ISHC Senior Award in Heterocyclic Chemistry (2007), the August-Wilhelm-von-Hofmann-Denkmünze Award (Germany, 2008), the Chandler Medal, Columbia University (2008), Lampousa Lifetime Achievement Award (Cypriot American Association) (2009); the Science Award, Ministry of Education and Culture, Cyprus (2010), the Benjamin Franklin Medal in Chemistry (2011), the Rolf Sammet Guest Professorship (Germany, 2014), the Nemitsas Prize (Cyprus, 2014), the Einstein Professorship (China, 2014), the ‘MAN of the Year’ Award (Cyprus, 2015), Scientist of the Year Award (Cyprus, 2015), Phileleftheros Award (Cyprus, 2015), and the Wolf Prize (Israel, 2016).

Nicolaou is a Member of the New York Academy of Sciences (1987), Fellow of the American Academy of Arts and Sciences (1993), Member of the National Academy of Sciences (USA, 1996), Fellow of the American Association for the Advancement of Science (1999), Foreign Member of the Academy of Athens (Greece, 2001), Honorary Fellow of the Indian Academy of Sciences (2007), Honorary Member of the Israel Chemical Society (2009), Member of the German Academy of Sciences Leopoldina (2009), Honorary Life Fellow of the Singapore National Institute of Chemistry (2011), Member of the American Philosophical Society (2011), Foreign Member of the Royal Society of London (2013), and Member of the National Academy of Inventors (2015). He holds 10 honorary degrees from universities around the world.

He is the author or co-author of more than 790 scientific articles, reviews, and book chapters, 79 patents, and five books, including the popular Classics in Total Synthesis co-authored with his student E.J. Sorensen (1996, VCH), Classics in Total Synthesis II co-authored with his student S.A. Snyder (2003, Wiley-VCH), Classics in Total Synthesis III co-authored with his student J.S. Chen (2011, Wiley-VCH), and Molecules That Changed the World, co-authored with his research associate T. Montagnon (2008, Wiley-VCH). His dedication to chemical education is evidenced by his training of hundreds of graduate students and postdoctoral fellows.

Research Areas

Organic Synthesis; Chemical Biology


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