TY - JOUR
T1 - Design and synthesis of indol-2-one derivatives as potential RET inhibitors
AU - Li, Zhenzhu
AU - Sun, Kai
AU - Xu, Yuanhong
AU - Zhu, Fuli
AU - Mao, Zhenyu
AU - Wang, Yang
AU - Yuan, Yaxia
AU - Qiu, Ting
AU - Chen, Xiabin
AU - Ma, Lei
N1 - Publisher Copyright:
© 2023 Elsevier Ltd
PY - 2023/12/15
Y1 - 2023/12/15
N2 - 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.
AB - 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.
KW - Cell proliferation
KW - Indol-2-one
KW - RET kinase inhibitors
KW - Structure-activity relationship
KW - Structure-based optimization
UR - http://www.scopus.com/inward/record.url?scp=85179685538&partnerID=8YFLogxK
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U2 - 10.1016/j.bmcl.2023.129538
DO - 10.1016/j.bmcl.2023.129538
M3 - Article
AN - SCOPUS:85179685538
SN - 0960-894X
VL - 97
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
M1 - 129538
ER -