Editorial [Hot Topic: Recent Advances in the Solid-Phase Organic Synthesis of Biologically Interesting Compounds (Executive Editor: Ernesto G. Mata)]

Solid-phase chemistry has been used for the synthesis of organic molecules for more than 30 years. However, this powerful approach remained unappreciated until the work by Bunin and Ellman in 1992 on solid-phase synthesis of arrays of 1,4-benzodiazepine-2-ones. Similar work on other drug-like molecules followed and a major revival in the study of solid-phase organic synthesis (SPOS) began. For developing high throughput synthesis, chemistry on a solid support is attractive from different perspectives: (i) filtration can be used for rapid purification; (ii) excess reagents can be used so the reactions can be driven to completion; (iii) automation is easily accomplished; and (iv) relative site isolation is achieved getting the "pseudo-dilution effect" which makes intramolecular macrocyclization a suitable reaction that could be carried out efficiently on solid-phase rather than in solution. Nowadays, combinatorial synthesis of small organic molecules using solid-phase approaches is recognized as a powerful tool for the rapid development of novel lead compounds and for the optimization of therapeutic efficacy. The present issue of Mini-Reviews in Medicinal Chemistry consists of eight invited review articles that cover different areas of research dealing with the application of SPOS to the preparation of biologically interesting compounds. The first article of this issue by A. Ganesan describes recent achievement of his group in different aspects of solid-phase synthesis including synthesis of unsymmetrical guanidines, tetrahydro-β-carbolines and kahalalide A. In the next article, Cironi, Alvarez and Albericio present an overview of recent examples of the use of chemistry on solid support in the preparation of non-peptidic natural products and related compounds. In the third article, gives an update on the application of solid-phase methodologies for the preparation of biologically interesting compounds containing hydroxamic acid moiety. The fourth article by Poirier and Maltais provides a comprehensive review on the solid-phase synthesis of steroidogenic enzyme inhibitors and steroid receptor modulators. Next, Kamal and colleagues contribute with two reviews dealing with the recent advances in the solid-phase synthesis of benzodiazepines in their first article, and quinoxaline, quinazoline and benzimidazole in their second article. In the seventh article, Pettersson, Clotet-Codina, Este, Borrell and Teixido give a compilation of the combinatorial methodologies applied to the development of anti-HIV drug. In the final article, we provide an update on the application of solid-phase and combinatorial synthesis to the preparation of β-lactam compounds. Finally, I would like to express my sincere thanks to the authors, all experts in their fields, for setting aside time to write these excellent reviews that give prestige to this issue. It has been an honor for me to work with such outstanding scientists. I fully anticipate that their effort will be appreciated by the scientific community interested in this important area of research.