Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell’s natural …

Hyperactive signaling of the MAP kinase pathway resulting from the constitutively active B-Raf
V600E mutated enzyme has been observed in a number of human tumors, including …

Leucascandrolide A (1) was isolated from the sponge Leucascandra caVeolata by Pietra
and co-workers in 1996. 1 The natural product displays strong in vitro cytotoxicity against KB …

Heterobifunctional PROTAC degraders are gaining attention as a differentiated therapeutic
modality with the potential for oral dosing in the clinic. Belonging to the beyond Rule of Five …

The Smoothened receptor (Smo) mediates hedgehog (Hh) signaling critical for development,
cell growth, and migration, as well as stem cell maintenance. Aberrant Hh signaling …

… Hornberger a , Jeffrey R. Jackson b , Kevin W. Kuntz a , Timothy J. … KH Hornberger, JG
Badiang, JM Salovich, KW Kuntz, KA Emmitte, M. Cheung … Kuntz, K.; Salovich, J.; Mook, R.; …

Aniline ‘headgroups’ were synthesized and incorporated into an alkynyl thienopyrimidine
series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular …

The scope of Pd-catalyzed synthesis of N-Boc-protected anilines from aryl bromides and
commercially available tert-butyl carbamate is described. For the first time, this process can be …

A one-pot synthesis of disubstituted benzimidazoles from 2-nitroanilines is described.
Hydrogenation of N-substituted 2-nitroanilines with palladium on carbon as catalyst in the …

A novel class of substituted pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines has been identified
that are potent and selective inhibitors of both EGFR/ErbB-2 receptor tyrosine kinases. …