As anticancer agent

Pnor to 1975, discussions of fluonnatcd pharmaceuticals focused mainly on anti-mflammatory steroids, antipsychotic phenothiazines, and 5-fluorouraciI and Its derivatives as anticancer agents [/ 2] Dunng the past 25 years, and especially in the last decade, tluonnated dmgs have been marketed for the treatment of a wide variety of diseases This section will focus on those presently marketed drugs where the presence of fluonne has produced significant therapeuhc advantages... 

Chemicals with antiandrogenic activity inclnde pharmacenticals developed as anticancer agents (e.g., flntamide, Neri and Monahan 1972 Neri et al. 1972, in Lntsky et al. 1975) and 179-methyltestosterone nsed to treat testosterone deficiency (Katsiadaki et al. 2006). Other antiandrogens inclnde varions pesticides snch as the... 

In 1985, it was reported by Hsiang et al. [43] that the cytotoxic activity of 20-(S)-camptothecin (CPT III) was attributed to a novel mechanism of action involving the nuclear enzyme topo I, and this discovery of unique mechanism of action revived the interest in CPT and its analogues as anticancer agents. CPT stabilizes the covalent, reversible topo I-DNA complex leading to the inhibition of DNA synthesis in mammalian cells and interferes with the topo I breakage-reunion reaction [44]. Clinical trials and structure-activity relationships have demonstrated the requirement of the a-hydroxy group, the... 

Ravelo, A. G. Estevez-Braun, A. Chavez-Orellana, H. Perez-Sacau, E. Mesa-Siverio, D. Recent studies on natural products as anticancer agents. Curr. Top. Med. Chem. 2004, 4, 241-265. 

Dervan PB, Poulin-Kerstien AT, Fechter EJ, Edelson BS (2005) Regulation of Gene Expression by Synthetic DNA-Binding Ligands. 253 1-31 Dias N, Vezin H, Lansiaux A, Badly C (2005) Topoisomerase Inhibitors of Marine Origin and Their Potential Use as Anticancer Agents. 253 89-108 DiMauro E, see Saladino R (2005) 259 29-68... 

Acharya MR, Sparreboom A, Venitz J, Figg WD (2005) Rational development of histone deacetylase inhibitors as anticancer agents a review. Mol Pharmacol 68 917-932... 

Drummond DC, Noble CO, Kirpotin DB, Guo Z, Scott GK, Benz CC (2005) Clinical development of histone deacetylase inhibitors as anticancer agents. Annu Rev Pharmacol Toxicol 45 495-528... 

Labarre, J.-F. Up to-date Improvements in Inorganic Ring Systems as Anticancer Agents. 102, 1-87 (1982). 

These phytochemicals are common in the Asteraceae (Compositae) and Apiaceae (Umbelliferae) (Chitwood, 1992 Zidom et al., 2005). There is considerable interest in these compounds because of their potential as anticancer agents and therapeutic agents (e.g. Zheng et al., 1999 Kobaek-Farsen... 

Faivre, S., Kroemer, G., and Raymond, E. (2006). Current development of mTOR inhibitors as anticancer agents. Nat. Rev. Drug Discov. 5, 671-688. 

Combretastatins are a class of compounds originally derived from the African Willow tree (Combretum caffrum) and are powerful reversible inhibitors of tubulin polymerization. This class of molecules has been shown to bind to the colchicine binding site of tubulin, by the same mode of action as mentioned above (Sect. 1.2). Combretastatins consist of a ris-slilbcnc core structure. To date, there have been several compounds that have shown promise as potential anticancer drugs. However, development of these compounds as anticancer agents is limited by issues of chemical stability, bioavailibilty, toxicity, and solubility. 

Antiemetic drugs, 27 (1990) 297 Antifilarial benzimidazoles, 25 (1988) 233 Antifolates as anticancer agents, 25 (1988)... 

Two TV-nitrosoureas, Bischloroethyl-nitrosourea (BCNU) and l-chloroethyl-3-cyclohexyl-1-nitrosourea (CCNU), have been used as anticancer agents in clinics but their mechanism and their toxicities have yet to be determined78. 

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