Add time:07/22/2019         Source:sciencedirect.com

Publisher SummaryNitrogen mustards were among the earliest drugs to be used for systemic cancer treatment. An enormous amount of information has become available on their chemistry and their mechanisms of interaction with DNA and on the spectrum of their biological activities in living systems. There have been relatively few clinically useful mustard-based anticancer drugs developed in the last few decades. The usefulness of mustards as cytotoxins has never been in question. The difficulty has always been to deliver them in a tumor cell selective fashion. This chapter describes three relatively new ways in which more selective targeting of mustards is being attempted. The work on DNA targeting has already resulted in the development of tallimustine (20) for clinical trial. It seems likely that the work now proceeding on hypoxia-selective ADEPT and GDEPT (genedirected enzyme-prodrug therapy) prodrugs using mustards as effectors will also result in new mustards for clinical evaluation.

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