Design and biological evaluation of substituted 5,7-dihydro-6H-indolo[2,3-c]quinolin-6-one as novel selective Haspin inhibitors

• Main Authors: Sreenivas Avula (Author), Xudan Peng (Author), Xingfen Lang (Author), Micky Tortorella (Author), Béatrice Josselin (Author), Stéphane Bach (Author), Stephane Bourg (Author), Pascal Bonnet (Author), Frédéric Buron (Author), Sandrine Ruchaud (Author), Sylvain Routier (Author), Cleopatra Neagoie (Author)
• Format: Book
• Published: Taylor & Francis Group, 2022-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

A library of substituted indolo[2,3-c]quinolone-6-ones was developed as simplified Lamellarin isosters. Synthesis was achieved from indole after a four-step pathway sequence involving iodination, a Suzuki-Miyaura cross-coupling reaction, and a reduction/lactamization sequence. The inhibitory activit...