No abstract

Recently we created the novel indolylprodigiosin derivative 2 (obatoclax) and demonstrated its ability to antagonize multiple members of the B-cell lymphoma (Bcl) family of antiapoptotic proteins. The compound has shown potent anticancer activity in several animal tumor models. Obatoclax is now in Phase 1b and 2 clinical trials directed against multiple hematologic and solid tumor malignancies. To support its clinical development, a new scalable synthesis was required. Obatoclax has been prepared using a three-step synthesis, starting from commercially available 4-methoxy-3-pyrrolin-2-one. The reaction sequence involves a haloformylation reaction followed by a Suzuki cross-coupling reaction with an indole-2-boronic acid. The synthesis is completed by an acid-mediated condensation with 2,4-dimethyl-1H-pyrrole.

No abstract

No abstract

A Facile Synthesis of C 2 -Symmetric 17β-Estradiol Dimers. -(RABOUIN, D.; PERRON, V.; N'ZEMBA, B.; C.-GAUDREAULT, R.; BERUBE*, G.; Bioorg. Med. Chem. Lett. 13 (2003) 3, 557-560; Dep. Chim.-Biol., Univ. Quebec, Trois-Rivieres, Que. G9A 5H7, Can.; Eng.) -F. Santoso 18-172