David Festus Charles Moffat

TL;DR: The src-family protein kinase inhibitors as mentioned in this paper are selective inhibitors of protein kinases, and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate kinase action is believed to have a role.

TL;DR: Pyrimidines of formula (1) are described wherein Ar is an optionally substituted aromatic or heteroaromatic group; R 1 is a hydrogen atom or a straight or branched chain alkyl group, R 2 is a -X1-R3 group where X1 is a direct bond or a linker atom or group.

TL;DR: In this paper, a general formula for protein tyrosine kinase inhibitors is described, where Ar is an optionally substituted aromatic group, R 2 is a hydrogen or halogen atom or a group, X 1-R2a where X 1 is a direct bond or a linker atom or group, and R 2a is an alternatively substituted straight or branched chain alkyl, alkenyl or alkynyl group.

TL;DR: A novel series of HDAC inhibitors demonstrating class I subtype selectivity and good oral bioavailability and one compound, 21r, showed good oral activity in these models, including dose-related activity in a LoVo xenograft and showed good activity in combination with other anticancer agents in in vitro studies.

TL;DR: This work demonstrates selective delivery of many types of intracellularly targeted small molecules to monocytes and macrophages by attaching a small esterase-sensitive chemical motif (ESM) that is selectively hydrolyzed within these cells to a charged, pharmacologically active drug.