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Design and synthesis of indol-2-one derivatives as potential RET inhibitors. | LitMetric

Design and synthesis of indol-2-one derivatives as potential RET inhibitors.

Bioorg Med Chem Lett

Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China. Electronic address:

Published: October 2023

We synthesized and assessed five series of indol-2-one derivatives for their potential as RET kinase inhibitors. Notably, compounds B3, B6, D1, D2, D3, and D5 demonstrated significant inhibitory activity. Among these, D5 exhibited the best activity of inhibiting RET kinase, which provided reference for the subsequent development of RET kinase inhibitors as anti-thyroid cancer chemical.

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Source
http://dx.doi.org/10.1016/j.bmcl.2023.129538DOI Listing

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