August 2022 Molecules of the Month Runners-up
You’ve read about the top 10 molecules with publications from August, but what about the ones we found interesting that didn’t make it into Molecules of the Month? There were five runners-up from August 2022, including: a highly selective, dihydropyrimidinone-based CSF1R switch-control kinase inhibitor a non-competitive, allosteric CXCR1/2 inhibitor with inflammation-independent antinociceptive effects a drug…
July 2022 Molecules of the Month Runners-Up
You’ve read about the top 10 molecules with publications from July, but what about the ones we found interesting that didn’t make it into Molecules of the Month? There were six runners-up this month, including a selective covalent K-Ras(G12S) inhibitor with a butyrolactone warhead, a κ opioid receptor agonist, and a dinucleotide STING agonist. You…
First Disclosures from EFMC-ISMC Nice, 2022
This year’s EFMC-ISMC conference in Nice, France, had a fantastic collection of talks. Among the highlights were the two First Disclosure sections, where companies shared the structures of their latest clinical candidates for the first time. Many thanks to Dr. Julien Lefranc, one of our featured reviewers, for sharing his notes on these sessions. We’ll…
First Disclosures from ACS Chicago 2022
We’re here at ACS Chicago 2022, covering sections of particular interest to drug discovery scientists. Among the highlights are the First Disclosures sections, where companies are sharing structures of clinical candidates for the first time. We’ll go more in-depth into the science from the conference soon – for now, here’s a high-level summary: Structure of…
Lenacapavir Synthesis Highlights
In this guest article, Dr. Luíza Cruz breaks down the synthesis of Gilead’s lenacapavir (GS-6207), Drug Hunter’s Small Molecule of the Year – 2020. Lenacapavir is a promising first-in-class, long-acting injectable (LAI) HIV capsid inhibitor. Interesting synthetic steps employed in this route include an unusual sodium chlorite-mediated benzylic oxidation, efficient installation of the gem-difluoro moiety,…
June 2022 Molecules of the Month Runners-Up
Readers have been asking for more molecules, so we started a new feature that highlights a few of the molecules we liked that didn’t make it into Molecules of the Month. There were six runners-up this month, including an orally available ALK2 inhibitor and a direct AMPK activator for X-linked adrenoleukodystrophy. You can read more…