Martin Kramer

TL;DR: Developmental pathways in neural crest cells that have a direct bearing on melanoma formation are highlighted.

TL;DR: A series of N-alkyl-5-(1H-benzimidazol-1-yl)thiophene-2-carboxamides with low nanomolar in vitro potency against DHODH demonstrated good tolerability and oral exposure in the mouse, and ED50 values in the 4-day murine P. berghei efficacy model resulted in sterile cure.

TL;DR: Using a target-based high throughput screen, a series of potent, species-specific inhibitors of P. falciparum DHOD are identified and validated as an antimalarial drug target and provide chemical scaffolds with which to begin medicinal chemistry efforts.

TL;DR: The discovery of a novel antimalarial agent using phenotypic screening of Plasmodium falciparum asexual blood-stage parasites is described and Optimized compound 27 has an excellent off-target activity profile in erythrocyte lysis and HepG2 assays and is stable in human plasma.

TL;DR: The synthesis and structure-activity relationship of a series of 5-(2-methylbenzimidazol-1-yl)-N-alkylthiophene-2-carboxamides that are potent inhibitors against PfDHODH but do not inhibit the human enzyme are reported.