Over the past decade, there has been a rising interest in the use of carboranes as a potential pharmacophoric moiety in the development of new drugs for the treatment of various types of cancer. The unique physical and chemical properties of carboranes make their use attractive in drug development. In several instances, the inclusion of carboranes into a drug structure has increased the agent's binding affinity, potency, or bioavailability. The purpose of this review is to highlight applications of carboranes to the medicinal chemistry of cancer. erwise rapidly metabolize [5]. Furthermore, selective chemical substitution of each carbon or boron atom in these clusters allows for their use as rigid, three dimensional scaffolds upon which to construct new drug molecules.Nearly all past biomedical research involving carboranes has focused on their use in the design of boron delivery agents for boron neutron capture therapy (BNCT)[2]. This binary radiation therapy depends on the selective delivery of a high concentration of boron-10 atoms to targeted tissues. It is generally accepted that a minimum concentration of 30 ppm is required for successful BNCT therapy and this concentration is equivalent to the delivery of approximately 10 9 boron atoms to each targeted cell. As BNCT human clinical trials have been attempted nearly continuously for the past five decades, there is a large body of literature associated with the use of carboranes for the development of BNCT boron agents. There are several good reviews and books covering that work [6][7][8][9][10][11][12][13]. While BNCT requires the delivery of large quantities of boron to diseased tissue, (requiring concentrations of boron in the low millimolar range) there is an increasing interest to use carboranes to synthesize new and highly potent drugs which operate at the opposite extreme of the concentration range, namely nanomolar, to picomolar.Ortho-carborane and its carbon-functionalized derivatives may be prepared by reacting acetylene (or functionalized acetylene) with the decaborane derivative B 10 H 12 L 2 , where L is a weak Lewis base [3,14]. The acetylenes used in these reactions include a wide range of functional groups such as esters, halides, carbamates, ethers, and nitro groups; however, such reactions are not successful in the presence of
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