Targeted chemical libraries: the keys to unlock the ubiquitin system Is novel chemistry the final frontier for ubiquitin system drug discovery?

By Dr Jason Brown and Dr J. Mark Treherne
Although the widespread use of target-focused libraries has led to the rapid expansion of novel chemistry as research tools in drug discovery to exploit many classes of drug target, the u...

Chemical space, high throughput screening and the world of blockbuster drugs.

By Dr Hakim Djaballah
Spring 2013
We are constantly told that if a high throughput screen does not identify hit(s) then blame it on the compounds in your library. The community has accepted this notion and unleashed a che...

Carbon-14 labelled API manufacturing.

By Dr Sean L. Kitson and Dr David Speed
Winter 2012/13
Carbon-14 labelled API and IMP requirements for Phase 0/I to Phase III mass balance and micro-dosing clinical trials can be met by contract manufacturing in compliance with MHRA and FDA P...

Keeping ahead of the flow: Can the next generation of flow chemistry and biology platforms be fully integrated to transform the efficiency of small-molecule drug discovery for pharmaceutical industry?

By Dr J Mark Treherne, Dr David M Parry and Christopher N Selway
Summer 2011
There have been many false dawns in small-molecule drug discovery, promising individual technologies and integrated platforms to improve the efficiency of drug discovery. Although high-th...

Custom Carbon-14 Radiolabelling: investing to meet new challenges.

By Dave Roberts
Winter 2009
One consequence of an increasing demand from regulators for robust quantitative data on the behaviour of new drugs in man and for information on the fate of pharmaceuticals in the environ...

Overcoming the limitations of chemical structure.

By Dr Andy Vinter, Dr Steve Gardner and Dr Sally Rose
Summer 2009
The pharmaceutical business has been profoundly hampered by a ubiquitous and unexpected obstacles; the way it draws its chemical compounds. Scientists, patent agents and business decision...

Microwave-Assisted Orgainc Synthesis - an Enabling Technology with Disruptive Potential.

By Dr Anil Vasudevan
Fall 2008
Since the original publications on the benefits of conducting organic reactions in a microwave by Gedye1 and Majetich2 in the mid-80s, the uptake of this technique was sluggish at best fo...

Zebrafish: a versatile in vivo model for drug safety assessment.

Dr Wendy Alderton and Dr St phane Berghmans
Fall 2006
Safety pharmacology has become an integral part of non-clinical safety assessment for new chemical entities in the past two decades1.The relative novelty of this discipline has granted it...

Medicinal Chemistry: progress through innovation.

By Dr Terry Hart
Summer 2006
Medicinal chemistry is a specialised science that has evolved to encompass a broad range of disciplines concerned with the identification, synthesis and development of drug-like compounds...

Microwave-assisted synthesis in the pharmaceutical industry a current perspective and future prospects.

By Dr Richard Wagner
Summer 2006
In the past five years there has been a dramatic upsurge in the use of microwave heating within the pharmaceutical industry to facilitate the chemical synthesis of new chemical entities.T...

The Role of the Medicinal Chemist in the Drug Discovery Process: current status and future prospects.

By Dr Stevan W Djuric
Winter 2005
The need for the pharmaceutical industry to produce a constant stream of new NCEs has never been more paramount but with constantly changing R&D paradigms what is the role of the modern m...

Radiosynthesis; a vital role supporting drug development?

By Dave Roberts and Professor Bill Lockley
Fall 2004
The key in vivo drug metabolism and pharmacokinetic studies continue to be undertaken using radiolabelled versions of drug molecules. Traditionally, the preparation of these isotopically ...

SCAVENGER strategies in organic synthesis.

By Professor Peter Wipf and Dr Claire M. Coleman
Spring 2004
Part 1 of this article (DDW,Winter 2003/4) discussed the fundamental principles of the use of scavenging techniques in combinatorial and organic synthesis. In this article, more recent de...

SCAVENGER strategies in organic synthesis.

By Professor Peter Wipf and Dr Claire M. Coleman
Winter 2003
Over the past 20 years combinatorial chemistry has proved to be an important tool for the generation of large numbers of compounds required for drug discovery programmes.This two-part art...