Perhaps this paper is showing its age, but at the time BMCL papers were basic, with just a table of two of measurements and simple synthesis. Non the less, this is the paper describing the discovery of a candidate drug (1) that went on to become the product Gleevec (Imatinib); this first tyrosine kinase inhibitor (the Wikipedia page has more data). The drug made quite an impact on many patients lives. Looking back, with experienced eyes, we can see the structural features now present in ATP binding pocket kinase inhibitors. The research process was rational and screened multiple kinases, leading by careful SAR analysis to 1. Tne compound, which is quite selective, in part due to the methyl group on the central ring. Of note is the ‘pan’ kinase inhibitor 9 – this compound might be worth adding to your compound collections, such that early screening could yield a tool compound?
Imatinib – Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives
#BucketListPapers #DrugDiscovery #MedicinalChemistry #BeTheBestChemistYouCanBe