Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck — a selectivity insight

Molecular interdiction of Src-family kinase signaling in hematopoietic cells

“…The resulting molecules are 100-fold more potent than PP1 at inhibiting TCR-stimulated IL-2 synthesis in Jurkat T cells. Interestingly, these compounds have been further elaborated to generate orally active agents capable of inhibiting IL-2 production in vivo (Burchat et al, 2002).…”

Pyrrolopyrimidine: A Versatile Scaffold for Construction of Targeted Anti-cancer Agents

“…6,25,26 Pyrrolopyrimidines have been reported to bind to the Tie-2 kinase domain (Figure 2) [27][28][29] However, no specific details were available with regard to Tie-2 kinase/cellular potency, selectivity, SAR, ADMET and in vivo attributes. Later on there have been several reports on non-pyrrolopyrimidine based Tie-2 inhibitors 30,31 but few showed kinase selectivity at the time.…”

Making Sense of Structures by Utilizing Mother Nature's Chemical Libraries as Leads to Potential Drugs

“…31 During the study, the first natural product inhibitor of Tie-2 kinase was reported 32 {19} (see Figure 21 of the same class of kinases. [33][34][35][36] Current details of the evolution and utility of this approach as an integrated program have been provided in two recent reviews by the Waldmann group, and these should be consulted for the specific details of the processes involved. 37, 38…”