Chem92_William%20Fenical

Chem92_William%20Fenical - The Growing Role of the Oceans...

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Unformatted text preview: The Growing Role of the Oceans in the Treatment of Cancer William Fenica and Co workers William Fenical and Co-workers Center for Marine Biotechnology and Biomedicine Scripps Institution of Oceanography Rebecca and John Moores Cancer Center Skaggs School of Pharmacy and Pharmaceutical Science University of California San Diego University of California, San Diego La Jolla, CA Nature - The Traditional Source for Drug s- Used for over 3000 years.- Traditional medicines common today in many parts of the world.- Many natural anti- cancer drugs have cancer drugs have been used in China and elsewhere. Natural Products in Drug Discovery I. - Over 150 of the drugs in current use are of natural origin. II. - Natural Products are the most successful source for agents for the treatment of cancer. III Terrestrial sources are the most traditional but III. - Terrestrial sources are the most traditional, but since ca. 1980 marine environments have proven to be superior. IV. - The NCIs Experimental Therapeutics Group has led a world-wide search for new anti-cancer drugs. NCI has supported academic programs (NCDDGs) in this area. The Oceans and Biodiversity- The oceans are more than 70% of the earths surface- The oceans are our most biodiverse environment with 34 of the 36 known phyla represented. Drug Discovery Successes - Tropical Marine Invertebrates Ascidian Diazona sp . Philippines Diazonamide A - Tumor Growth Inhibition N HN H H OH O O H N N HO N O Cl NH Cl O Diazonamide A OH H Diazonamide A IC 50 = 18 nM at 24 hour exposure * Joint project between Hlne Vervoort, Gerrit Los and Stephen Howell, UCSD Cancer Center Ascidian Diazona sp. Philippines- Show potent in vitro cytotoxicity: 3 nM vrs HCT-116 colon carcinoma - An inhibitor of mitotic cell division (G2 / M) N HN H N H N C OH- Possible target: tubulin ( in vitro data)- Specific mechanism looks interesting (novel tubulin binding site, E. Hamel) O O H N HO N O Cl NH Cl O- Unrelated, structurally, to any other drug candidate known. OH N H HO- Conclusion: active lead compound - Problem is supply! Unfortunately, not yet advanced to preclinical stage- Now a synthesis is available allowing the drug to go forward. (2007) Soft-Coral Eleutherobia sp . - Australia- This is a soft-coral, a member of the class Alcyonaceae. It is related distantly to the hard corals, but they are completely soft bodied and lack physical defenses.- Crude extract shows potent in vitro cytotoxicity: 10 ng/mL vrs HCT-116. Thomas Lindel Soft-Coral Eleutherobia sp . - Eleutherobin O OH OH O O O N N CH 3 OH O O OCH 3 O- Following cytotoxicity as a guide, the cytotoxin Eleutherobin was isolated from the crude organic extract....
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Chem92_William%20Fenical - The Growing Role of the Oceans...

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