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Cover Legend: KC Nicolaou 299-300 31/12/2008 02:46 ÌÌ ™ÂÏ›‰·1 INTERNATIONAL JOURNAL OF ONCOLOGY 34: 299-300, 2009 1 Cover legend: K.C. Nicolaou; a member of The Editorial Academy of The International Journal of Oncology compounds for ring closure reactions was complemented by the introduction of new reagents such as N-phenylseleno- succinimide (NPS) and N-phenylselenophthalimide (NPSP). These selenium reagents were shown to induce a number of diverse reactions such as phenylselenolactonizations, phenyl- selenoetherifications, and 1,2-phenylselenohydroxylations. Discovered during a program in total synthesis, these powerful reactions were subsequently used by Nicolaou, as well as others, to synthesize numerous natural product analogs, including stable prostacyclins and other biologically important compounds. This early example of interdisciplinary research at the interface of chemistry and biology was augmented by the molecular design and chemical synthesis of novel prostacyclin and thromboxane analogs such as carboprostacyclin, pinane thromboxane A2 and carbocyclic thromboxane A2, which K.C. Nicolaou was born on July 5, 1946, in Cyprus, where he greatly facilitated biological studies in the eicosanoid field. grew up and went to school until the age of 18. In 1964, he Indeed, from the very start of his career, Nicolaou began went to England, where he spent two years learning English to weave together the themes of total synthesis of natural and preparing to enter the university. He studied chemistry at products, the development of new synthetic methods and the University of London (B.Sc., 1969, Bedford College, First technologies, and explorations in chemical biology as a Class Honors; Ph.D. 1972, University College, with Professors cohesive and integrated research philosophy. This approach F. Sondheimer and P.J. Garratt). In 1972, he moved to the to science has served well the fields of chemistry, biology and United States and after postdoctoral appointments at Columbia medicine, while simultaneously providing training to students University (1972-1973, Professor T.J. Katz) and Harvard in the art of chemical synthesis, preparing them for academia University (1973-1976, Professor E.J. Corey) he joined the or industrial research. faculty at the University of Pennsylvania, where he rose Using his interwoven approach to chemical synthesis, a through the ranks to become the Rhodes-Thompson Professor number of accomplishments have been made, with the total of Chemistry. In 1989, he accepted joint appointments at the syntheses of the following molecules representing perhaps University of California, San Diego, where he is Distinguished his highest achievements: endiandric acids (plant metabolites, Professor of Chemistry, and The Scripps Research Institute 1982), efrotomycin (antibiotic, 1984), amphotericin B (anti- I where he is the Chairman of the Department of Chemistry fungal agent, 1987), calicheamicin Á1 (anticancer drug, 1992), and holds the Skaggs Professorship of Chemical Biology and rapamycin (anticancer and immunosuppressive drug, 1993), the Darlene Shiley Chair in Chemistry. Taxol® (top-selling anticancer drug, 1994), zaragozic acid A K.C. Nicolaou's Ph.D. work (F. Sondheimer and P.J. (cholesterol-lowering agent, 1994), brevetoxins B and A Garratt, University College London) dealt with the synthesis (marine neurotoxins, 1995 and 1998), epothilones A and B and study of cyclic diallenes and dicumulenes. During his (anticancer drugs, 1997), eleutherobin (antitumor agent, postdoctoral stint at Columbia (T.J. Katz) he explored the 1998), vancomycin (antibiotic of last resort, 1999), the CP chemistry of benzvalene, and in the course his postdoctoral molecules (cholesterol-lowering agent, 1999), sanglifehrin A stay at Harvard (E.J. Corey) he worked on various projects in (immunosuppressant, 1999), bisorbicillinoids (antioxidants, organic synthesis. It was during this latter appointment that 1999), colombiasin A (cytotoxic agent, 2001), apoptolidin he (and Corey) developed the 2-pyridylthiol macrolactonization (antitumor agent, 2001), hybocarpone (cytotoxic agent, 2001), method (double activation method) and participated in the coleophomones B and C (antibiotics, 2002), diazonamide A total synthesis of various natural and designed molecules, (antitumor agent, 2002, 2003), 1-O-methyllateriflorone (cyto- including erythronolide B and prostaglandin analogs. toxic agent, 2003), azaspiracids-1, -2, and -3 (marine neuro- K.C. Nicolaou's independent career began with the toxins, 2004-2006), thiostrepton (antibiotic, 2004), the bis- development of organoselenium-based methodology for the anthrquinones epi-cytoskyrin and regulosin (cytotoxic and anti- construction of various heterocycles, including lactones, viral agents, 2005), abyssomicin C and atrop-abyssomicin C ethers and amines. The exploration of PhSeCl and related (antibiotics, 2006), marinomycins A-C (antibiotics, antitumor 299-300 31/12/2008 02:46 ÌÌ ™ÂÏ›‰·2 INTERNATIONAL JOURNAL OF ONCOLOGY 34: 299-300, 2009 agents, 2006), GE2770A and GE2770T (antibiotics, 2006), Medal, Universitat Zurich (Switzerland, 2000), Foundation platensimycin (antibiotic, 2006), uncialamycin (antitumor (Germany, 2001), the Centenary Medal, Royal Society of antibiotic, 2007), biyouyanagin A (anti-HIV agent, 2007), Chemistry (UK, 2000-2001), the Ernst Schering Prize, Ernst and platencin (antibiotic, 2008). Among these, Taxol® serves Schering Research Foundation (Germany, 2001), the Nagoya as his most celebrated and widely recognized triumph. Indeed, Gold Medal of Organic Chemistry, Nagoya University (Japan, considered as the ‘holy grail’ of synthesis in the late 1980s 2001), the Tetrahedron Prize for Creativity in Organic and early 1990s, this extraordinary molecule stands as the Chemistry (2002), the ACS Nobel Laureate Signature Award quintessential symbol of all natural products molecular for Graduate Education in Chemistry (2003), the Aristeio complexity, and its total synthesis as the single most important Bodossaki Prize (Greece, 2004), the ACS A.C. Cope Award milestone of complex molecular construction in recent decades. (2005), Auburn Section, American Chemical Society, G.M. Besides the total synthesis of the anticancer drug Taxol® Kosolapoff Award (2006), the Burkardt-Helferich Prize in 1994, Nicolaou's research in the cancer area resulted in the (2006), the ISHC Senior Award in Heterocyclic Chemistry design and synthesis of several antitumor agents, some of (International, 2007), the August-Wilhelm-von-Hofmann- which are currently in preclinical and clinical development. Denkmünze Award (Germany, 2008), and the Chandler His total syntheses are characterized by elegant synthetic Medal, Columbia University (2008). strategies, and often accompanied by discoveries of new Nicolaou is a Member of the New York Academy of synthetic technologies, while his designed molecules serve as Sciences (1987), Fellow of the American Academy of Arts useful biological tools. and Sciences (1993), Member of the National Academy of For his scientific work, Professor Nicolaou has received Sciences (USA, 1996), Fellow of the American Association numerous awards and honors, including the Humboldt for the Advancement of Science (1999), Foreign Member, Foundation US Senior Scientist Prize (Germany, 1987), the Academy of Athens (Greece, 2001), and holds 12 honorary A.C. Cope Scholar Award, American Chemical Society degrees from universities around the world. (1987), the Award for Creative Work in Synthetic Organic He is the author or co-author of almost 700 scientific Chemistry, American Chemical Society (1993), the Dr. Paul articles, reviews, and book chapters, over 60 patents, and 4 Janssen Prize for Creativity in Organic Synthesis, Janssen books, including the popular Classics in Total Synthesis, co- Research Foundation (Belgium, 1994), the Rhone-Poulenc authored with his student Erik J. Sorensen (1996, VCH), Medal, Royal Society of Chemistry (UK, 1995), the William Classics in Total Synthesis II, co-authored with his student H. Nichols Medal, New York Section-American Chemical Scott A. Snyder (2003, Wiley-VCH), and Molecules That Society (1996), the Inhoffen Medal, Gesellschaft fur Bio- Changed the World, co-authored with his research associate technologische Forschung mbH (GBF) (Germany, 1996), the T. Montangon (2008, Wiley-VCH). Fully illustrated in color, Ernest Guenther Award in the Chemistry of Natural Products, his latter book aims to inspire young students into the sciences American Chemical Society (1996), the Chemical Pioneer and inform everyone of the impact of chemistry and molecules Award, American Institute of Chemists (1996), the Linus on society. His dedication to chemical education is evidenced Pauling Award, Oregon, Portland, Puget Sound Sections- by his training of more than 400 graduate students and post- American Chemical Society (1996), the Decoration of the doctoral fellows. Order of the Commander of Honor Medal (bestowed by the In summary, Nicolaou has made significant contributions President of Greece, 1998), the Esselen Award for Chemistry to the art and science of total synthesis. His work impacted in the Public Interest, American Chemical Society (1998), on chemistry, biology and medicine. the Yamada Prize (Japan, 1999), the first Aspirin Prize for He lives in La Jolla, California, with his wife Georgette, Solidarity through Chemistry (Spain, 1999), the Max Tishler with whom he has four children, Colette, Alex, Christopher Lecture Prize, Harvard University (2000), the Paul Karrer Gold and PJ..
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