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1949stone

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[资源] Privileged Scaffolds in Medicinal Chemistry Design, Synthesis, Evaluation

Preface
Privileged scaffolds – when I was approached two years ago by the RSC editorial board to edit a book on this topic, I was immediately thrilled as it was very timely.
I would like to quote from an interview given by Brent Stockwell, one of the leading figures in drug discovery:
‘‘In 1957, during a cleanup of his lab at the pharmaceutical company Roche, Sternbach discovered an old flask containing a chemical he had
synthesized previously, but discarded for lack of interest. On a lark, he decided to have it tested for its anti-anxiety potential, a therapeutic area
he had become interested in. The chemical, of an unknown identity, had striking anti-anxiety activity that was superior to the existing marketed
drugs of that era. Within three years, Sternbach was able to figure out the identity of the chemical and had it approved for use in patients – a remarkable success, considering that drug development nowadays takes 10 to 15 years. This chemical was the first of the benzodiazepines, a class
of drugs with a specific shape and structure that is powerful for treating anxiety. Some years later, Ben Evans and his colleagues at Merck
discovered that benzodiazepine derivatives were also effective in treating other diseases and in interacting with other types of proteins. He suggested that this class of molecules is privileged, in the sense that it is especially effective at interacting with proteins and altering the course of
disease. Other privileged molecular structures have since been discovered, and these molecules might be the key to addressing the undruggable proteins. Since these privileged compounds are so effective at interacting with numerous classes of proteins, they may be an effective
starting point to look for new drugs against the supposedly undruggable protein targets.’’
With this notion in mind, I asked a number of colleagues both in industry and academia to give their own opinion for a given compound class. In all cases, a short overview into syntheses is given.
The book is organized by compound classes with a general lead-in and a chapter addressing computational approaches. It should be noted that
during the preparation, the Baell/Holloway paper in Science (2014) addressing ‘‘Pan Assay Interference Compounds - PAINS’’ was published, which is also a very valuable source for addressing privileged structures from a toxophoric standpoint.
Stefan Bra¨se
Karlsruhe Institute of Technology
Germany

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2017-05-09 18:55:19, 13.65 M