Demeunynck M., Bailly C., Wilson W.D. Small Molecule DNA and RNA Binders: From Synthesis to Nucleic Acid Complexes

Wiley-VCH Verlag GmbH & Co. KGaA, 2003. — 732 p. — ISBN: 3-527-30595-5The ultimate goal of most organic-medicinal chemists is to see the small molecule that they have synthesized become a useful drug for the treatment of human diseases. Unfortunately, even with modern technology this is an extremely rare event. In most cases, the compounds designed and synthesized (generally with pain and passion) have a brief existence that does not exceed the first biological activity assay. The valley between chemistry and therapeutics is deep and difficult to cross but nevertheless the two disciplines are intimately associated. It is our goal to help construct a bridge between the makers of the small molecules and the users. Over the past two decades, a relatively large number of useful anticancer and antiparasitic drugs have been discovered or rationally designed based on the principle of nucleic acids recognition. A better understanding of the molecular rules that govern interactions between small molecules and the many sequences and structures of DNA and RNA is pivotal to the development of novel drug candidates. How does the drug adapt to the nucleic acid target (and vice versa)? How do nucleic acid structures affect ligand binding? How do small molecules read the genetic information? These types of questions continue to excite our scientific curiosity and the quest for better DNA/RNA binders drives modern researchers much as the search for the Holy Grail did the ancients.