Abstract
AbstractRAS proteins are necessary for cell survival, and their mutations are closely related to tumor formation and progression. Mutated RAS proteins were undruggable owing to their smooth surface decades ago. Since chemists found that covalently binding to mutated cysteine (G12 C) was a potential therapy for KRASG12C inhibition. Recently, AMG‐510 and MRTX‐849 were approved in 2021 and 2022 respectively for solid tumor treatment. In this paper, started with KRASG12C inhibitor ARS‐1620, we introduced different hydrophilic fragment on it and reached compound K09, which had the best KRASG12C inhibitory activity and antiproliferation activities. Compound K09 is regarded as a lead compound for further exploration.
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