Immunogenic
cell death (ICD) is a way of reengaging the tumor-specific
immune system. ICD can be induced by treatment with chemotherapeutics.
However, only a limited number of drugs and other treatment modalities
have been shown to elicit the biomarker responses characteristic of
ICD and to provide an anticancer benefit in vivo. Here, we report
a rationally designed redox-active Au(I) bis-N-heterocyclic carbene
that induces ICD both in vitro and in vivo. This work benefits from
a synthetic pathway that allows for the facile preparation of asymmetric
redox-active Au(I) bis-N-heterocyclic carbenes.
A copper-catalyzed selective C-N cross-coupling has been developed based on chelation-assisted amidation of readily available aryl boronic acids at room-temperature under open-flask conditions. The reaction is scalable and tolerates a wide spectrum of functional groups delivering fully substituted unsymmetrical amides in high yields (up to 96%). The C-N cross coupling also established with aryl silanes, extending the palette of coupling partners of this strategy.
Isoquinoline-based polycyclic lactams such as isoindoloisoquinolinones, pyrroloisoquinolinones, and benzo[a]quinolizinones were successfully assembled from the corresponding imides by using a TfOH-mediated (TfOH = trifluoromethanesulfonic acid) imide carbonyl activation and cyclization strategy. By employing this simple method, the isoquinoline
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