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Discovery of 1-(arylacetyl)-2-phenyl-pyrrolidine Derivatives as Novel POLθ-pol Inhibitors via Structure-Based Virtual Screening and Fragment Fusion

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DNA polymerase theta (POLθ) has been regarded as a promising therapeutic target for the treatment of BRCA-deficient tumors. In this study, 1-(arylacetyl)-2-phenyl-pyrrolidine derivative VS-13 was identified as a POLθ-pol inhibitor hit with an IC50 value of 1... ...