Tesirine intermediate-1 is the intermediate of Tesirine . Tesirine (SG3249), a pyrrole benzodiazepine (PBD) dimer, is a DNA small channel crosslinker with strong cytotoxicity. Tesirine can be used to synthesize Antibody-Drug Conjugates (ADCs), the warhead component of the payload is SG3199 , which has strong anticancer cell activity.
References:
[1]. Howard, et al. Process for the preparation of intermediates useful for the synthesis of pyrrolobenzodiazepine dimers. World Intellectual Property Organization, WO2013053872 A1. 2013-04-18. [2]. Tiberghien AC, et al. Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016;7(11):983-987. Published 2016 May 24.