Michal Lebl
J. Comb. Chem., 1999, 1, 1, 3-24
https://doi.org/10.1021/cc9800327

Abstract

It is appropriate to start this new journal with an article about the history of this particular fieldsespecially when the field is so new that even the basic terminology is not completely defined.† When I was asked to write an article about the history of combinatorial chemistry, I believed that it would not be too difficult since I was engaged in this exciting new technology from the start of the first combinatorial chemistry company, Selectide Corporation in Tucson. To make this historical retrospective more objective, I decided to consult with several scientists who published in this field at the early stages and whose articles may be considered as having formed the new way of thinking about the techniques used to develop new drugs and catalysts and an unlimited variety of materials. After reading the responses of my colleagues, it was clear that when we were building Selectide in 1991, there were scientists already heavily engaged in creating and using diversity in various forms. Some people were exploring this new field without even realizing it. I can document this fact from my own experience. In 1988, we published a paper with Giorgio Fassina and Irwin Chaiken1 in which we synthesized a mixture of analogues of oxytocin by coupling a mixture of amino acids in one step of the synthesis and applying this mixture to the column with immobilized neurophysin. The analogues with an affinity toward neurophysin were retained on the column, and after elution their structures were analyzed. None of us realized the potential of this technique for the development of new drugs; at that time we were “entrenched” in the approach of making one compound at a time, analyzing it, and evaluating it biologically. However, even in the 1990s the world was not ready to accept the idea of building libraries of organic molecules and screening them to find interesting compounds. It took another several years before an academic course of combinatorial chemistry was offered to students at The University of Louisville in 1996 by Professor Arno Spatola.