Antibody-Drug Conjugates with Pyrrole-Based KSP Inhibitors as the Payload Class.

The number of cytotoxic payload classes successfully employed in antibody-drug conjugates (ADCs) is still rather limited. The identification of ADC payloads with a novel mode of action will increase therapeutic options and potentially increase the therapeutic window. Herein, we describe the utilization of kinesin spindle protein inhibitors (KSPi) as a novel payload class providing highly potent ADCs against different targets, for instance HER-2 or TWEAKR/Fn14.

Enantiopure 2-substituted glyceraldehyde derivatives by aza-Claisen rearrangement or C-alkylation of enamines.

2-Alkyl derivatives of butane-2,3-diacetal (BDA) protected glyceraldehyde were stereoselectively prepared by aza-Claisen rearrangement of N-allyl-enammonium ions or C-alkylation of enamines. This allows rapid and convenient access to densely functionalized chiral building blocks.

Synthetic glycopeptides from the mucin family as potential tools in cancer immunotherapy.

Compared to glycoproteins of healthy cells, glycoproteins of tumor cells are often aberrantly glycosylated. Thus, glycopeptide fragments of surface glycoproteins of tumor cells are of interest as tumor-associated antigens for the distinction between normal and tumor cells. Cancer immunotherapy directed at selectively targeting these tumor-associated glycoprotein structure alterations--deficient glycosylation and, thus, exposure of peptide epitopes which are masked in normal cells--is considered a promising approach for the treatment of cancer.