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Science Gifts 2014: Books on Drug Discovery and Medicinal Chemistry

Today I wanted to highlight books specifically on medicinal chemistry and drug discovery. Those are always festive additions to the holiday season, right? This list builds on last year’s recommendations, with updated editions of some titles, and adds a number of suggestions from readers.
I’ll start out with a recent history of our whole field: The Evolution of Drug Discovery. There are a lot of good books written at various levels about the discovery of particular drugs or therapies, but it’s rare to see the entire business of drug discovery looked at in this way.

For general medicinal chemistry, you have Bob Rydzewski’s Real World Drug Discovery: A Chemist’s Guide to Biotech and Pharmaceutical Research. A recent addition to this area is Drug Discovery: Practices, Processes, and Perspectives, by Jack Li and E. J. Corey. Another recommendation is Textbook of Drug Design and Discovery by Krogsgaard-Larsen et al. Several readers here have recommended earlier verions of Silverman’s medicinal chemistry book, and there’s now a third edition: The Organic Chemistry of Drug Design and Drug Action. Readers have also recommended Camille Wermuth’s The Practice of Medicinal Chemistry. For getting up to speed, several readers recommend Graham Patrick’s An Introduction to Medicinal Chemistry. Similarly, Medicinal Chemistry: The Modern Drug Discovery Process is a recent introductory textbook that I thought was well done.

Process chemistry is its own world with its own issues. Recommended texts here are Practical Process Research & Development by Neal Anderson, Repic’s Principles of Process Research and Chemical Development in the Pharmaceutical Industry, and Process Development: Fine Chemicals from Grams to Kilograms by Stan Lee (no, not that Stan Lee) and Graham Robinson. On an even larger scale, McConville’s The Pilot Plant Real Book comes recommended by readers here, too.

Case histories of successful past projects can be found in Drugs: From Discovery to Approval by Rick Ng and also in Walter Sneader’s Drug Discovery: A History.

Another book that focuses on a particular (important) area of drug discovery is Robert Copeland’s Evaluation of Enzyme Inhibitors in Drug Discovery. Other recent books on particular areas of med-chem are Bioisosteres in Medicinal Chemistry by Brown et al., recommended by several readers, Scaffold Hopping in Medicinal Chemistry, and Protein-Protein Interactions in Drug Discovery, Volume 56

For chemists who want to brush up on their biology, readers recommended an earlier edition of this now updated Terrence Kenakin book: A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery , as well as Pharmacology in Drug Discovery: Understanding Drug Response. Cannon’s Pharmacology for Chemists, and Molecular Biology in Medicinal Chemistry by Nogrady and Weaver have also been recommended.

Overall, one of the most highly recommended books across the board comes from the PK end of things: Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization by Kerns and Di. This one is from 2008, but the same authors have another book coming out in February: Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs. Another recent PK-centric book is Lead Optimization for Medicinal Chemists. For getting up to speed in this area, there’s Pharmacokinetics Made Easy by Donald Birkett, and the Drug Metabolism and Pharmacokinetics Quick Guide has also been recommended.

In a related field, standard desk references for toxicology seems to be Casarett & Doull’s Toxicology: The Basic Science of Poisons and Hayes’ Principles and Methods of Toxicology Every medicinal chemist will end up learning a good amount toxicology, too often the hard way.

And a recently mentioned book here might prove useful as well: Navigating the Path to Industry, aimed at academic scientists (not just entry-level ones, either) who are looking at industrial research positions and wondering how to get from here to there.
As always, suggestions for more titles to add to the list are welcome.

10 comments on “Science Gifts 2014: Books on Drug Discovery and Medicinal Chemistry”

  1. dearieme says:

    “aimed at academic scientists (not just entry-level ones, either) who are looking at industrial research positions”: which industries should they choose. Not pharma, obviously.

  2. johnnyboy says:

    Targeted more to the general public, but going to a sometimes surprising level of scientific precision, is The Emperor of all Maladies, by Siddhartha Mukherjee. It’s an eminently readable and informative work on cancer.

  3. Anonymous BMS Researcher says:

    Interesting list; I’ll take a closer look over the holidays. Since I’ll be traveling by air, I’m a lot more likely to purchase titles available in electronic format: bits won’t add mass to my luggage, and I’ll have Internet access where I’m going.
    I concur with the recommendation of Kerns and Di Drug-like Properties; there’s a copy of that one in my office. Good summary of many issues that regularly come up in Working Group Meetings.

  4. Erebus says:

    “Blood-Brain Barrier in Drug Discovery” sounds like an interesting book. There are very few works on this topic — and the ones I’ve read were less than complete, to say the least.
    I second your recommendation of Copeland’s “Evaluation of Enzyme Inhibitors in Drug Discovery”. It’s a very valuable book — and not just for people working on enzyme inhibitors. It contains a succinct and very valuable review of ADME and Tox.
    The CRC Press just released an interesting book called “Nanotechnology and Drug Delivery, Volume One: Nanoplatforms in Drug Delivery”, which sums up nanomedicine’s current state of the art. The formulation folks who read this blog might be interested.

  5. Anonymous says:

    When will we get to see “Things I Will Not Work With: The Book” by Derek Lowe?

  6. Douglas Kell says:

    I know it’s a Cinderella subject for some…, but REALLY no books on drug transporters?? How do you think drugs ACTUALLY get into cells (hint: http://journal.frontiersin.org/Journal/10.3389/fphar.2014.00231/abstract)? Meanwhile, try:
    1. Bhardwaj, R.K., Herrera-Ruiz, D.R., Xu, Y., Carl, S.M., Cook, T.J., Vorsa, N., and Knipp, G.T. (2008) Intestinal transporters in drug absorption. In Biopharmaceutics Applications in Drug Development (Krishna, R. and Yu, L., eds), pp. 175-261, Springer.
    2. Delespaux, V. and de Koning, H.P. (2012) Transporters in antiparasitic drug development and resistance. In Antiparasitic and antibacterial drug discovery: trypanosomatidae (Flohe, L., et al., eds), pp. in press, Wiley-Blackwell.
    3. Ecker, G. and Chiba, P., eds (2009) Transporters as drug carriers: structure, function, substrates. Wiley/VCH.
    4. Fromm, M.F. and Kim, R.B., eds (2011) Drug Transporters. Springer.
    5. Ishikawa, T., Kim, R.B., and König, J., eds (2013) Pharmacogenomics of Human Drug Transporters: Clinical Impacts Wiley.
    6. Sugiyama, Y. and Steffansen, B., eds (2013) Transporters in Drug Development: Discovery, Optimization, Clinical Study and Regulation. AAPS/Springer.
    7. Thompson, T.N. (2011) The Clinical Significance of Drug Transporters in Drug Disposition and Drug Interactions. In Pharmacokinetics in Drug Development, Vol 3: Advances and Applications (Bonate, P.L. and Howard, D.R., eds), pp. 285-313, Springer.
    8. You, G. and Morris, M.E., eds (2014) Drug Transporters: Molecular Characterization and Role in Drug Disposition. Wiley.

  7. Anonymous BMS Researcher says:

    I also look forward with great eagerness to the “Things I won’t work with” book. Will some pedantic editor “up with which Derek will not put” (as Churchill might say) try to change its title to “Things with which I will not work”?

  8. Anonymous BMS Researcher says:

    For those still in grad school, this book is highly recommended. IF (1) it had existed in the 1980s, (2) my adviser had thrown it at me, (3) I had read it, and (4) above all I had actually followed its advice THEN my time to degree might have been shortened.
    Getting What You Came For: The Smart Student’s Guide to Earning an M.A. or a Ph.D., by Robert Peters, 1997
    However, by the time it came out, I already was a Doctor of Philosophy!

  9. Doug Steinman says:

    A little bit far afield from med chem but, I think, useful to a medicinal chemist working in the pharmaceutical industry are the books written by Sherwin Nuland who was a Professor of Surgery at Yale. “How We Live” and “How We Die” are particularly good and provide a fascinating look at the treatment of patients. After all, that is our ultimate goal as medicinal chemists. The books are interesting and well written.

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