PubMed · 14249929
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O HRDY. 1964. [DEXAMETHASONE].. https://pubmed.ncbi.nlm.nih.gov/14249929/
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The success rate of discovering new polymorphs by crystallization from solution may be increased if solvents with diverse properties are used during initial polymorph screening. In this study, eight solvent parameters, including hydrogen bond acceptor propensity, hydrogen bond donor propensity, polarity/dipolarity, dipole moment, dielectric constant, viscosity, surface tension and cohesive energy density (equal to square of solubility parameter), of 96 solvents were collected. Using the cluster statistical analysis of the parameters, these 96 solvents were separated into 15 solvent groups. Such solvent groups may provide guidelines for the judicious choice of solvents with diverse properties for polymorph screening.
Medicinal chemists are frequently asked to review lists of compounds to assess their drug- or leadlike nature and to evaluate the suitability of lead compounds based on their "attractiveness" and/or synthetic feasibility as a basis for launching a drug-discovery campaign. It is often felt that one medicinal chemist's opinion is as good as any other, but is it? In an attempt to answer this question, an experiment was performed in conjunction with a recent compound acquisition program (CAP) conducted at Pharmacia. Historically, the CAP included a review of many thousands of compounds by medicinal chemists who eliminate anything deemed undesirable for any reason. In a review conducted in 2002, about 22 000 compounds requiring review by medicinal chemists were broken down into 11 lists of approximately 2000 compounds each. Unknown to the medicinal chemists, a subset of 250 compounds, previously rejected by a very experienced senior medicinal chemist, was added to each of the lists. Most of the 13 medicinal chemists who participated in this process reviewed two lists, although some only reviewed a single list and one reviewed three lists. Those compounds that were deemed unacceptable were recorded and tabulated in various ways to assess the consistency of the reviews. It was found that medicinal chemists were not very consistent in the compounds they rejected as being undesirable. The inconsistency arises from the subjective analysis that all humans utilize when considering "data sets" of any kind. This has important implications for pharmaceutical project teams where individual medicinal chemists review lists of primary screening hits to identify those compounds suitable for follow-up. Once a compound is removed from a list, it and other structurally similar compounds are effectively removed from further consideration. This can also have an impact on computational chemists who are developing models for assessing the desirability or attractiveness of different classes of compounds for lead discovery.
Stephen Neidle was educated at Imperial College, London, where he graduated in chemistry and then proceeded to do a PhD in crystallography. After a period as an ICI Fellow, he joined the Biophysics Department at King's College, which ignited his interest in nucleic acid structural studies. He was appointed as one of the first Cancer Research Campaign Career Development Awardees, becoming a Life Fellow on moving to the Institute of Cancer Research. He was appointed to the Chair of Biophysics at the Institute of Cancer Research in 1990, and moved to the new Chair of Chemical Biology at the School of Pharmacy in the University of London in 2002, where he also directs the Cancer Research UK Biomolecular Structure Group. He is currently Chairman of the Chemical Biology Forum of the Royal Society of Chemistry, which is involved in developing the interface between chemistry and the life sciences. He will shortly assume the Directorship of the newly-established Centre for Cancer Medicines at the School. Stephen Neidle has received several awards for his work on drug-nucleic acid recognition and drug design, including the 2000 prize of the Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry, and its 2002 Interdisciplinary Award. He was the 2004 Paul Ehrlich Lecturer of the French Societé de Chimie Therapeutique, and was recently awarded the 2004 Aventis Prize in Medicinal Chemistry.