DOI: 10.3390/reactions6010020 ISSN: 2624-781X
Design and Synthesis of 7-(N-Aryl Pyrrolidinyl) Indoles as Potential DCAF15 Binders
Ravi Devarajappa, Scarlett Kiyeleko, Sofiane Hocine, Victor Cosson, Remi Calandrino, Timea Baló, Jayson Alves Bordelo, Sébastien Triboulet, Laure Caruana, Laurence Klipfel, Sandrine Calis, András Herner, Stephen HanessianWe describe the design and synthesis of a series of 7-(N-aryl pyrrolidinyl) indoles and oxo-analogs as isosteric mimics of the DCAF15 binder E7820, a well-known member of aryl sulfonamides known as SPLAMs. The functionalization of C-7 in indoles was achieved by metal-catalyzed CH-activation with unexpected results. Binding assays revealed the pyrrolidine N-aryl carboxylic acid analog to be as equally active as E7820.