Next-generation epidermal growth factor receptor (EGFR) inhibitors against the d746-750/T790M/C797S mutation were discovered through two-track virtual screening and de novo design. A number of nanomolar inhibitors were identified using 2-aryl-4-aminoquinazoline as the molecular core and the modified binding energy function involving a proper dehydration term, which provides important structural insight into the key principles for high inhibitory activities against the d746-750/T790M/C797S mutant. Furthermore, some of these EGFR inhibitors showed a greater than 1000-fold selectivity for the d746-750/T790M/C797S mutant over the wild type, as well as nanomolar activity against the mutant.
A strategy for visible-light-induced
site-selective C–H
acylation of pyridinium salts was developed by employing N-methoxy- or N-aminopyridinium salts, offering a
powerful synthetic tool for accessing highly valuable C2- and C4-acylated
pyridines. The methoxy or amidyl radicals photocatalytically generated
from the pyridinium salts can undergo hydrogen atom abstraction from
readily available aldehydes to form acyl radicals, which can engage
in addition to pyridinium substrates. Remarkably, the use of N-methoxypyridinium salts preferentially gives the C2-acylated
pyridines, and the site selectivity can be switched from C2 to C4
by using N-aminopyridinium salts. The utility of
this transformation was further demonstrated by the late-stage functionalization
of complex biorelevant molecules and by application of acyl radicals
to photocatalytic radical cascades.
In this paper, our aim is finding the term of generalized Euler polynomials. We also obtain some identities and relations involving the Bernoulli numbers, the Euler numbers and the Stirling numbers.
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