Synthesis and Biological Evaluation of a Carbamate-Containing Tubulysin Antibody-Drug Conjugate.

Antibody-drug conjugates (ADCs) use antibodies to deliver cytotoxic payloads directly into tumor cells via specifically binding to the target cell surface antigens. ADCs can enhance the anti-tumor effects of antibodies, and increase the delivery of cytotoxic payloads to cancer cells with a better therapeutic index. An ADC was prepared with a potent carbamate-containing tubulysin analogue attached to an anti-mesothelin antibody via a Cit-Val dipeptide linker.

Bis{μ-4,4',6,6'-tetra-tert-butyl-2,2'-[N-(2-oxidoeth-yl)imino-dimethyl-ene]diphenolato}dialuminium(III).

The title compound, [Al(2)(C(32)H(48)NO(3))(2)], exists as a dimer with bridging ethoxide groups. It was isolated from a reaction mixture of the parent ligand and trimethyl-aluminium in tetra-hydro-furan. The geometry around the Al(III) atom is a slightly distorted trigonal-bipyramid, typical of atrane derivatives.