Indolactam dipeptides as nanomolar Gli inhibitors was written by Mendoza, Manuel;Tran, UyenPhuong;Zhang, Grace C.;Leister, Jeffrey;To, Kyle;Malepeai-Tofaeono, Theodore;Ondrus, Alison E.;Billingsley, Kelvin L.. And the article was included in ACS Medicinal Chemistry Letters in 2022.Recommanded Product: 128-08-5 This article mentions the following:
The Gli transcription factors within the Hedgehog (Hh) signaling pathway play essential roles in human development. However, the reactivation of Gli proteins in adult tissue is tumorigenic and drives the progression of several cancers, including the majority of basal cell carcinomas. Here we describe a novel set of indolactam dipeptides that target protein kinase C (PKC), exploiting the unique capacity of PKC isoenzymes to act as regulators of Gli. We devised an efficient synthetic route for the indolactam-based natural product (-)-pendolmycin and a series of analogs, and we evaluated these analogs in mechanistically distinct Gli reporter assays. The lead compound from these studies, N-hexylindolactam V (I), exhibits superior Gli suppression relative to clin. inhibitors and blocks the growth of Gli-dependent basal cell carcinoma cells. More broadly, our structure-activity studies provide inroads for the development of novel Gli antagonists and new avenues for combating Gli-driven cancers. In the experiment, the researchers used many compounds, for example, 1-Bromopyrrolidine-2,5-dione (cas: 128-08-5Recommanded Product: 128-08-5).
1-Bromopyrrolidine-2,5-dione (cas: 128-08-5) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Recommanded Product: 128-08-5
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary