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Pure Appl. Chem., 2012, Vol. 84, No. 7, pp. 1479-1542

Published online 2012-06-26

Analogue-based drug discovery: Contributions to medicinal chemistry principles and drug design strategies. Microtubule stabilizers as a case in point (Special Topic Article)

Mohammad H. El-Dakdouki1 and Paul W. Erhardt2*

1 Department of Chemistry, Michigan State University, East Lansing, MI 48824, USA
2 Center for Drug Design and Development, University of Toledo, Toledo, OH 43606, USA

Abstract: The benefits of utilizing marketed drugs as starting points to discover new therapeutic agents have been well documented within the IUPAC series of books that bear the title Analogue-based Drug Discovery (ABDD). Not as clearly demonstrated, however, is that ABDD also contributes to the elaboration of new basic principles and alternative drug design strategies that are useful to the field of medicinal chemistry in general. After reviewing the ABDD programs that have evolved around the area of microtubule-stabilizing chemo-therapeutic agents, the present article delineates the associated research activities that additionally contributed to general strategies that can be useful for prodrug design, identifying pharmacophores, circumventing multidrug resistance (MDR), and achieving targeted drug distribution.