1207426-46-7Relevant articles and documents
Synthesis of indole inhibitors of silent information regulator 1 (SIRT1), and their evaluation as cytotoxic agents
Laaroussi, Hanna,Ding, Ying,Teng, Yuou,Deschamps, Patrick,Vidal, Michel,Yu, Peng,Broussy, Sylvain
, (2020)
A series of achiral indole analogues of the selective sirtuin inhibitor EX-527 (a racemic, substituted 1,2,3,4 tetrahydrocarbazole) was designed to stabilize the bioactive conformation, and synthesized. These new indoles were evaluated against the isolated sirtuin enzymes SIRT1 and SIRT2, and against a panel of nine human cell lines. Structure-activity relationship studies demonstrated the influence of the substituent at position 3 of the indole. The most potent SIRT1 inhibitor 3h, bearing an isopropyl substituent, was as potent as EX-527, and more selective for SIRT1 over SIRT2. Compound 3g, bearing a benzyl substituent, inhibited both sirtuins at micromolar concentration and was more cytotoxic than EX-527 on several cancer cell lines.
Microwave-assisted solid-acid-catalyzed friedel-crafts alkylation and electrophilic annulation of indoles using alcohols as alkylating agents
Kulkarni, Aditya,Quang, Phong,Toeroek, Bela
experimental part, p. 4010 - 4014 (2010/04/02)
Alcohols are considered environmentally benign alkylating agents since the only by-product generated in their reactions is water. Herein, we report a microwave-assisted Friedel-Crafts alkylation and electrophilic annulation of indoles using alcohols as al
