Over the past couple of decades, antibody–drug conjugates (ADCs) have revolutionized the
field of cancer chemotherapy. Unlike conventional treatments that damage healthy tissues …

Cyclopropane, epoxide, and aziridine groups are three-membered ring structural elements
found in a wide variety of natural products, some of which are depicted in Figure 1. 1 The …

Isatin (1H-indole-2, 3-dione) and its derivatives demonstrate a diverse array of biological
and pharmacological activities including anticonvulsant, antibacterial, antifungal, antiviral …

The de novo construction of enantioenriched 3-hydroxyindolenines and 3-oxindoles from
easily available starting materials has been highly desired. Herein, an enantioselectively …

Synthetic analogues of the DNA-alkylating cytotoxins of the duocarmycin class have been
extensively investigated in the past 40 years, driven by their high potency, their unusual …

Despite significant advances in treatment strategies over the past decade, selective
treatment of breast cancer with limited side-effects still remains a great challenge. The …

Epothilones A and B are naturally occurring microtubule-stabilizers, which inhibit the growth
of human cancer cells in vitro at nM or even sub-nM concentrations. In contrast to paclitaxel …

CC-1065, the duocarmycins and yatakemycin are members of a family of ultrapotent
antitumour antibiotics that have been the subject of extensive investigations due to their …

Pd/Cu‐catalyzed cross‐coupling of propargylamines with aromatic acyl chlorides (PdCl2,
CuI, Ph3P, 40–45° C) provides α‐aryl (hetaryl) aminoacetylenic ketones in a yield of up to …

A library of duocarmycin bioprecursors based on the CPI and CBI scaffolds was synthesized
and used to probe selective activation by cells expressing CYP1A1 and 2W1, CYPs known …