Derek Lowe's commentary on drug discovery and the pharma industry. An editorially independent blog from the publishers of Science Translational Medicine. All content is Derek’s own, and he does not in any way speak for his employer.
I hadn’t realized it, but there are some new elements that have been added to the “essential for biochemistry” list, and they’re a bit of a surprise. (I blogged about odd metals in biology a few years ago). I would guess that anything new at this point would be a surprise – the most recent… Read More
Here’s an update to a post from last year about silicon in drug-like molecules. The Denmark group at Illinois has investigated a range of silicon-containing heterocycles, providing both synthetic routes into the (mostly unknown) structures, and looking at some basic pharmaceutically relevant properties. There’s a lot of work in this pap… Read More
I like this review, but I’ve seen it before. Well, not this exact manuscript, but every few years it seems there’s another one with a similar title, something about “Incorporating Silicon Into Drug Structures”. I am guilty of the exact same thing, though: here’s a blog post from 2004 on the topic, and here’s one… Read More
So here’s a question for the medicinal chemists: how come we don’t like bromoaromatics so much? I know I don’t, but I have trouble putting my finger on just why. I know that there’s a ligand efficiency argument to be made against them – all that weight, for one atom – but there are times… Read More
Here’s the latest “medical periodic table”, courtesy of this useful review in Chemical Communications. Element symbols in white are known to be essential in man. The ones with a blue background are found in the structures of known drugs, the orange ones are used in diagnostics, and the green ones are medically useful radioisotopes… Read More
Now here’s a subject that most medicinal chemists have thought of at one point or another: why don’t I put a silicon into my compounds? Pretty much like carbon, at least when there’s only one of them, right? I’ve done it myself – I was working on a series of compounds years ago that had… Read More
There have been all kinds of boronic acid-based enzyme inhibitors over the years, but they’ve been mostly locked in the spacious closet labeled “tool compounds”. That’s as opposed to drugs. After all these years, Velcade is still the only marketed boron-containing drug that I know of. There’s been a good attempt to cha… Read More
You don’t see too many drugs with selenium in them, that’s for sure. It’s one of those elements that can be used to illustrate the Paracelsian doctrine that the dose makes the poison: selenium is an essential element that’s also toxic. There’s no doubt at all about either of those properties; it all depends on… Read More
When I wrote here about unknown compounds, using aza-steroids as examples, I apparently wasn’t thinking far enough afield. I noticed this new paper on a new class of tellura-steroids. I’ve no doubt that they’re new; probably no one has ever thought to make anything that looks quite like this before (there’s one other report… Read More
You know, I often think that I have too narrow a view of what kinds of structures can go into drug molecules. (That may come as worrisome statement for some past and present colleagues of mine, who feel that my tolerances are already set a bit too wide!) But I do have limits; there are… Read More
