The design, synthesis, and biological evaluation of PIM kinase inhibitors

PIM1 kinase inhibitors induce radiosensitization in non-small cell lung cancer cells

“…In addition, we monitored in the ITC experiments that tryptanthrin had relatively lower affinity to PIM1 than SGI-1776 and ETP-45299 (Table 1). To improve the potency against targets, a large number of inhibitors have been modified in their specific functional groups based on SAR studies [30,51,52]. Various substituents, including alkyl, O, S, N or cyclic moiety, would be applicable for better inhibitory efficacy of tryptanthrin against PIM1.…”

Potential Use of Selective and Nonselective Pim Kinase Inhibitors for Cancer Therapy

“…The resulting pan-Pim inhibitors exemplified by 14 ( Figure 4) showed good kinase selectivity, cellular potency, and good oral exposure. 54 Interestingly, the molecule displayed some CK2 inhibition, noted also for other Pim inhibitors in this series (vide infra). Scientists from Novartis reported the discovery of 15 and its analogues by structure-guided optimization of an HTS hit.…”

Synthesis and biological evaluation of new benzofuran carboxamide derivatives

“…Biological evaluation of new benzofuran carboxamide derivatives 5 hydroxide in ethanolic medium afforded the key intermediate 3 namely 3-amino benzofuran-2-carboxamide yielded 65%. Compound 4a was obtained by coupling of chloroacetyl chloride with compound 3 in 70% yield [38]. The regular nucleophilic substitution of different amines with compound 4a afforded the corresponding glycinamide based benzofuran derivatives (5a-j).…”