A concise synthesis of an alkylation subunit of the duocarmycins is achieved via a C–H-activation approach. The ethyl ester analogue of duocarmycin SA can be made in eleven linear steps from a commercially available precursor.
The natural product yatakemycin (YTM) is a potent antimicrobial DNA damaging agent. YtkR4 and YtkR5 are deoxyribonucleases that provide resistance to YTM toxicity by removing the a basic site produced by YtkR2 cleavage of a YTM-adenosine lesion.
Natural products (NPs) have long been foundational in medicine, from ancient herbal remedies to the discovery of transformative drugs like morphine and quinine.
Fc-glycan-specific ADC is a significant advance in site-specific ADCs for cancer therapy. Notably, JSKN003 and IBI343 have demonstrated promising results in phase 1 clinical trials and are advancing into phase 3 studies.
Chemodivergent synthesis of halogenated 1-pyrrolines, 3-azabicyclo[3.1.0]hex-2-enes and α,α-dibromo imines from N-allyl enamines via halide-controlled annulation.