Design and Synthesis of 7-(N-Aryl Pyrrolidinyl) Indoles as Potential DCAF15 Binders
We 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.
Authors
- Sébastien Triboulet
- Ravi Devarajappa (ORCID: https://orcid.org/0000-0002-9351-4849)
- Sofiane Hocine (ORCID: https://orcid.org/0000-0002-4241-3327)
- Scarlett Kiyeleko
- Stephen Hanessian (ORCID: https://orcid.org/0000-0003-3582-6972)
- András Herner
- Timea Baló (ORCID: https://orcid.org/0009-0009-4013-8243)
- Laurence Klipfel
- Victor Cosson
- Remi Calandrino
- Jayson Alves Bordelo
- Laure Caruana
Institutions
- Eötvös Loránd University (HU)
- University of California, Irvine (US)
- Servier (France) (FR)
- Université de Montréal (CA)
- Institut des Hautes Études Scientifiques (FR)
Publication Details
- Journal
- Reactions
- Published
- 2025-03-07
- DOI
- https://doi.org/10.3390/reactions6010020
- Citations
- 1
- Primary Topic
- Chemical Synthesis and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 0.81