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Medicinal Chemistry Books, 2019

I missed putting this up last year, but once again I have a list of medicinal chemistry books of interest. As in years past,  the list builds on previous recommendation posts, with updates and reader suggestions incorporated along the way.

For histories and broad overviews of the field, there have not been any recent additions. Earlier ones include 2011’s The Evolution of Drug Discovery, which still seems to be the biggest history of the field (its author, Jack Li also has a 2014 history of the industry, Blockbuster Drugs, looking at how things have been for previous last twenty years or so). There are case histories of individual drug projects to be found in Drugs: From Discovery to Approval by Rick Ng (2015 edition), and also in Walter Sneader’s Drug Discovery: A History. Longtime medicinal chemist Gene Cordes  published Hallelujah Moments: Tales of Drug Discovery in 2014.

In general medicinal chemistry, the whopper reference set of the field published a third edition recently: Comprehensive Medicinal Chemistry, edited by Sam Chackalamannil, Dave Rotella, and Simon Ward.  I don’t expect anyone to buy the >$4000 set off this blog link, but I’ll be very happy with the Amazon commission if you do. More reasonably for home use, a recommendation from several readers is Textbook of Drug Design and Discovery by Krogsgaard-Larsen et al. Jack Li has Medicinal Chemistry for Practitioners coming out early in 2020. A new third edition of Drug Discovery and Development has just been published, edited by James O’Donnell. Another recent title recommended by readers is Translating Molecules into Medicines, on drug development in general.A title from 2016 is  Small Molecule Medicinal Chemistry: Strategies and Technologies. From 2013, there’s Drug Discovery: Practices, Processes, and Perspectives, by (the prolific) Jack Li and E. J. Corey, and there’s also Bob Rydzewski’s Real World Drug Discovery: A Chemist’s Guide to Biotech and Pharmaceutical Research from 2008. Several readers here have also recommended earlier versions of Silverman’s medicinal chemistry book, now in its third edition: The Organic Chemistry of Drug Design and Drug Action. Readers have also recommended Camille Wermuth’s The Practice of Medicinal Chemistry, and it’s now in its fourth edition as of 2015. For getting up to speed, several readers recommend Graham Patrick’s An Introduction to Medicinal Chemistry (new edition as of 2017). Similarly, Medicinal Chemistry: The Modern Drug Discovery Process (Pearson Advanced Chemistry) is a recent introductory textbook that I found to be well written. Its author, Erland Stevens, runs a popular web-based med-chem training course as well.

More specific topics have their own monographs, such as the upcoming Fluorine in Life Sciences, A good one-stop-shop for fragment drug hunting is Fragment-Based Drug Discovery: Lessons and Outlook, and a related topic of interest is covered in the recent Biophysical Techniques for Drug Discovery. Similarly, there’s Advanced Methods in Structural Biology and NMR in Chemical Biology: Advances and Applications. A recent one (2017) is Practical Medicinal Chemistry with Macrocycles. On the thermodynamic side, there’s the recent Thermodynamics and Kinetics of Drug Binding. Other recent books that cover specific med-chem topics include Robert Copeland’s Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and Pharmacologists, which has gotten good reviews from readers here, Bioisosteres in Medicinal Chemistry by Brown et al. (also recommended by several readers), Scaffold Hopping in Medicinal Chemistry, Prodrugs and Targeted Delivery: Towards Better ADME PropertiesProtein-Protein Interactions in Drug Discovery, and the recent Allosterism in Drug Discovery. Chemical biology types may well be interested in the recent Chemoselective and Bioorthogonal Ligation Reactions, which is a fast-moving field as well as the newly published Target Discovery and Validation.

I have not noted many recent books on process chemistry and scale-up. A recent textbook is Chemical Projects Scale Up: How to Go From Laboratory to Commercial. Another reader-recommended book is Practical Process Research and Development – A Guide for Organic Chemists by Neal Anderson (2012). Repic’s Principles of Process Research and Chemical Development in the Pharmaceutical Industry is older (1998), but comes recommended as well. In the Oxford Chemistry Primers series, there’s Process Development: Fine Chemicals from Grams to Kilograms by Graham Robinson and Stan Lee (presumably not the Marvel Comics Stan Lee, a joke the author has surely heard once or twice), and Process Development: Physiochemical Concepts by John Atherton and Keith Carpenter.  The Pilot Plant Real Book by Francis McConville is subtitled “A Unique Handbook”, and it’s been recommended by readers with experience in that unique environment.

For chemists who want to brush up on their biology, Joseph Cannon’s Pharmacology for Chemists has also been recommended, and it looks like a completely new version has been published under the same title. Readers also recommended an earlier edition of this Terrence Kenakin book: A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, as well as his Pharmacology in Drug Discovery: Understanding Drug Response. A more advanced book on pharmacology, also reader-recommended, is Ehlert’s Affinity and Efficacy.

As has been the case for several years,  Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization by Kerns and Di, has been recommended by numerous readers as a textbook and reference (now in a 2016 edition). The same authors have also published Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs. I should note that there’s a new edition of Goodman and Gilman’s classic The Pharmacological Basis of Therapeutics, but I should also note that a review says that it’s had a good deal of useful material cut as compared to previous editions. More pharmacokinetics are to be found in Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. On the clinical end of things, a well-reviewed textbook is Concepts in Clinical Pharmacokinetics. For getting up to speed in this area in general, there’s Pocket Guide: Pharmacokinetics Made Easy by Donald Birkett, which will give you some background to understand what’s going on, and the Drug Metabolism and Pharmacokinetics Quick Guide, which has also been recommended. A recently updated textbooks is Clinical Pharmacokinetics and Pharmacodynamics.

In toxicology, the standard textbooks are Casarett & Doull’s Toxicology: The Basic Science of Poisons (now in a 2018 edition) and Hayes’ Principles and Methods of Toxicology (2014). Two weighty references are the Handbook of Toxicologic Pathology, and the more recently updated Comprehensive Guide to Toxicology in Nonclinical Drug Development (reader-recommended). Another book on toxicology in drug development is Preclinical Safety Evaluation of Biopharmaceuticals: A Science-Based Approach to Facilitating Clinical Trials, from 2008. There’s a new book in this field written for the educated-layman audience, Modern Poisons, which could well be interesting.

After posting the 2016 post in this series, readers also made suggestions for formulations. A recent entry in this field is Oral Formulation Roadmap (From Early Discovery to Development), and Pharmaceutical Preformulation and Formulation: A Practical Guide was also recommended. This is an area with a long list of increasingly specialized monographs available, so it’s hard to recommend further reading.

In general, statistics are a weak point with a lot of scientists. Jerrold Zar’s Biostatistical Analysis comes recommended by readers. For getting up to speed in this area, a well-reviewed textbook is Biostatistics: The Bare Essentials, and there’s also Essential Biostatistics: A Nonmathematical Approach. (As mentioned last time around, I remain curious how far a nonmathematical approach can take you in this area). A newly updated edition of Laboratory Statistics: Methods in Chemistry and Health Sciences has also been recently published.

Then there’s the informatics and computational field, and in these areas I hesitate to list anything more than just a few years old. Chemoinformatics For Drug Discovery was recommended as an introduction for those outside the field. Many other books in this area are starting to show their age, but a recent one is Applied Chemoinformatics: Tools and Methods. Bioinformatics has many other books choices as compared to chemistry. A recent introductory work is (appropriately) Introduction to Bioinformatics, and two computational resources are the R Bioinformatics Cookbook and the Bioinformatics with Python Cookbook.

That leads naturally to the broader computational chemistry field, where there’s the recently updated Introduction to Computational Chemistry, and In Silico Medicinal Chemistry, from Pipeline reader Nathan Brown. A new entry is Biomolecular Simulations in Structure-Based Drug Discovery. As for machine learning, I mentioned Deep Learning for the Life Sciences earlier this year as a good intro to the field,

For bridging the academia-industry gap, I can definitely recommend A Practical Guide to Drug Development in Academia, which has a lot of solid advice for academic researchers looking to get into the pharma world through their own research. I can also recommend Navigating the Path to Industry: A Hiring Manager’s Advice for Academics Looking for a Job in Industry. Both of these books are full of sound advice that people may find difficult to get elsewhere.

So that’s the list of

24 comments on “Medicinal Chemistry Books, 2019”

  1. Astounded says:

    go to craigslist boston and query for chemisty in the biotech/science section.

    Nothing…nada…zip, what a joke.

    You’re medicinal chemistry books aren’t good for much more than wiping your a## with these days

    1. loupgarous says:

      “You’re medicinal chemistry books aren’t good for much more than wiping your a## with these days

      Craiglist isn’t the best place to look for jobs requiring advanced college education. Or, apparently, jobs for people who know the difference between “your” and “you’re”.

  2. KazooChemist says:

    I checked the Amazon link to Comprehensive Medicinal Chemistry just for fun and I did get a good chuckle out of it. The image of the book’s cover shown in the listing is actually that of a book entitled “Long-term Performance and Durability of Masonry Structures”. Perhaps that chapter discusses all of the laboratory buildings that have been demolished after takeovers in Pharma. I know it would have a section on my home town.

    Derek: Where is the picture of the pie????

  3. Ray says:

    I’d love to get my hands on a few of these, but $250 for a book is just insane, especially on a grad student stipend. I’ve picked up a few old favorites for $50-80 on Amazon, but there is no second-hand market for a lot of these texts.

    I wonder how many copies of many of these books actually sold for full price. Industry folks, does your workplace have a library that keeps a copy of these books on hand? It is hard for me to see anyone picking a lot of these up even with a 15-25% author/editor discount, especially if they have literature access.

    1. Alexandra says:

      I know a Big Pharma company that gives its employees access to a comprehensive ebook library. But for a student most of these books are only accesible via a library.

      But there is a site similiar to our beloved paper sharing site that specializes on books. Searching around might help you.

    2. Pedwards says:

      It doesn’t work for all books, but abebooks often has academic books for cheap. You have to be fine with getting them used or the non-North American editions, but getting a $250 book for >$10 is worth it.

    3. Ken Sharp-Knott says:

      As a grad student you should take advantage of your university library. An astonishing number of these can be found available as electronic books viewable through your library catalog.

    4. d4T says:

      Libgen. Has pretty much every single one.

  4. Anonymous says:

    From a very limited amount of now outdated experience, I wonder if anyone has any estimates (or actual knowledge) of current financial arrangements between publishers and authors. In the past, extremely long hours of writing and editing to provide camera-ready or automatic typeset-ready material would result in high priced (read: “largely unaffordable”) books. The author/editors, who did almost everything but drive the delivery trucks to the post office or book stores, would see almost nothing.

    Which brings me to a secondary question: In the past, there were many printing presses in the US and Europe who could do the printing/binding/ etc-ing for the Big Publishers. Today, I have heard that many publishers have their printing / binding / etc-ing done in China at a much lower cost, even when you include the shipping and import costs of very heavy palettes of books. (I know someone who “vanity published” their own book, and ordered maybe 2000(?) 5000(?) copies. The actual final cost from China was less than half of the domestic US quoted cost.)

    1. cheap labor says:

      yup, and you can get a PhD chemist to work for peanuts over there too, he’ll sleep on a grass mat in front of his hood at night while the night shift chemist works.

      Pharma put all their faith in the Chinese, both here in the US and with outsourcing, the end result, small molecule chemistry programs have all but disappeared, try and find a job as a medicinal chemist these days….everyone’s linkedin profile says they’re “consulting”.
      It’s ridiculous, so many bright chemists graduating from good schools and good labs and yet all you see as far as staffing is people from overseas that can barely speak english and send every bit of IP they view to their buddies in an email attachment every night.

    2. Anonymouse says:

      Profit margins in the science publishing world are actually quite small. Print runs are very limited. How many people are interested in, or can understand pharm chemistry? Authors receive 10-15% of net sales in royalties, while publishers assume the expense and risk of the publishing process (editorial and graphic development, copy editing, page layout, accounting, printing, binding, etc.,) and distributors typically take 35%. Consequently a 10-15% profit margin sounds pretty good to a publisher’s ears. Look elsewhere for a “bad” capitalists.

    3. MrXYZ says:

      You are correct that a good deal of book printing has moved to China. I think this is particularly true for books that have large numbers of illustrations/images such as art books, field guides, and many science books. The US and Europe also still have some printing shops as well for these types of books. My understanding is that cost is one driver of where you go but that also the queue for getting things printed is quite long (year or two lead time) so that affects decisions.

      I know someone who has had books printed in China and, frankly, his opinion was quite positive. He was happy with the communications and with the quality of the product. The only thing that was a killer was the time difference.

      I know we hear a lot about outsourcing problems with China and all of the issues are worth taking seriously. On the other hand, we generally don’t hear from people who are very happy with the results they get when outsourcing to China (or other countries) so there is definitely sampling bias in these discussions.

  5. BargainHunter says:

    A saving of $3500 dollars on Comprehensive Medicinal Chemistry III ….

    Black Friday deal or what?!

  6. azetidine says:

    As far as using any of these books to help you actually put a drug on the market, you might as well buy a book on how to win the lottery, for all the good it will do you.

  7. SteveM says:

    Why trees are stilled felled to produce hard copy text books is beyond me.

    1. Pedwards says:

      Because some of us hate long-form reading on screens.

      1. Hap says:

        And because we’d actually like to be able to read it when we want and have it not disappear.

  8. AlloG says:

    I wrote a book once- A self-help book for trees- I called it “How not to become a book”

    I expect to sell 5 million copies.

    1. x says:

      Bad news – your target market was ground up for pulp to produce the books.

      1. AlloG says:

        How you know Dese things?

        1. loupgarous says:

          “How you know Dese things?”

          Dat should be “How u kno Dese tings?” You welcom.

  9. MedChemJournalClubber says:

    Would you have a couple of recommendations for reviews in the field that you would recommend to start with? E.g. for Bioisosters, I enjoy this work by Meanwell: https://pubs.acs.org/doi/10.1021/jm1013693. Let me know if you can think of other landmark papers that you would recommend for beginners in Medicinal Chemistry.

  10. Nathan Tumey says:

    I would add “Basic Principles of Drug Discovery and Development” by Benjamin Blass. We’ll be using this in a drug discovery class that I’m teaching this fall.

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