Cancer anticancer drugs

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Enediynes hold substantial promise as anticancer drugs because of their potency and selectivity. Not only do they inhibit cell growth, they have a greater tendency to kill cancer cells than they do normal cells. The mechanism by which enediynes act involves novel chemistry unique to the C C—C=C—C C unit, which leads to a species that cleaves DNA and halts tumor growth. 

Yart A, Mayeux P, Raynal P (2003) Gabl, SHP-2 and Other Novel Regulators of Ras Targets for Anticancer Drug Discovery. Curr Cancer Drug Targets 3 177-192... 

Camptothecin was discovered as an active anticancer drug isolated from the bark of Camptotheca acuminata. The anticancer activity of camptothecin was discovered in the 1960s by the National Cancer Institute (NCI) as part of a systematic effort to screen for novel anticancer agents derived from natural products. Monroe Wall and Mansuhk Wani identified the chemical structure of camptothecin. They also identified the chemical structure of taxol, again under the auspices of the NCI. Susan Hoiwitz was contracted by the NCI to elucidate the anticancer mechanisms of camptothecin. She found in the early 1970s that camptothecin induced DNA breaks and attested DNA and RNA synthesis. However, it is approximately 12 years later, only after DNA topo-isomerase I (Topi) had been identified in human cells, that Leroy Liu and his coworkers found that Topi was the cellular target of camptothecin [reviewed in [1]. 

Etoposide (XV) is a semisynthetic gylcoside derivative of podophyllotoxin, which is one of the most extensively used anticancer drugs in the treatment of various types of tumors [64,65]. The anticancer activity of this drug is mainly due to its ability to inhibit an ubiquitous and essential enzyme human DNA topo II [66,67]. Despite its extensive use in the treatment of cancers, it has several limitations, such as poor water solubility, drug resistance, metabolic inactivation, myelosuppression, and toxicity [68]. In order to overcome these... 

Stephen Hilton obtained his B.Sc. at King s College London in 1996 followed by a Ph.D. under the supervision of Professor Keith Jones and Dr Sheetal Handa. In 2002 he carried out a postdoctoral fellowship under the supervision of Professor William Motherwell at University College London. In 2006 he moved to his current position at The Institute of Cancer Research as a postdoctoral fellow in Medicinal Chemistry. His research interests lie in the area of natural products containing sulfur, radical chemistry and anticancer drug targets. 

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