Ohkanda, Junko; Strickland, Corey L.; Blaskovich, Michelle A.; Carrico, Dora; Lockman, Jeffrey W.; Vogt, Andreas; Bucher, Cynthia J.; Sun, Jiazhi; Qian, Yimin; Knowles, David; Pusateri, Erin E.; Sebti, Said M.; Hamilton, Andrew D. published the artcile< Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase>, SDS of cas: 16426-64-5, the main research area is structure design imidazole peptidomimetic inhibitor protein farnesyltransferase antitumor; Suzuki coupling imidazole peptidomimetic inhibitor protein farnesyltransferase antitumor.
A series of imidazole-containing peptidomimetic PFTase inhibitors and their co-crystal structures bound to PFTase and FPP are reported. The structures reveal that the peptidomimetics adopt a similar conformation to that of the extended CVIM tetrapeptide, with the imidazole group coordinating to the catalytic zinc ion. Both mono- and bis-imidazole-containing derivatives, 13 and 16, showed remarkably high enzyme inhibition activity against PFTase in vitro with IC50 values of 0.86 and 1.7 nM, resp. The peptidomimetics were also highly selective for PFTase over PGGTase-I both in vitro and in intact cells. In addition, peptidomimetics 13 and 16 were found to suppress tumor growth in nude mouse xenograft models with no gross toxicity at a daily dose of 25 mg·kg-1.
Organic & Biomolecular Chemistry published new progress about Antitumor agents. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, SDS of cas: 16426-64-5.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary