2. Academic Validation
  3. Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors

Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors

  • Bioorg Med Chem Lett. 2006 Apr 1;16(7):1846-9. doi: 10.1016/j.bmcl.2006.01.008.
Andrew Morrell 1,  Smitha Antony,  Glenda Kohlhagen,  Yves Pommier,  Mark Cushman
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA.
PMID: 16442283 DOI: 10.1016/j.bmcl.2006.01.008
Abstract

A method has been developed that relies on a two-step, one-pot condensation between phthalide and 2-carboxybenzaldehydes to provide benz[d]indeno[1,2-b]pyran-5,11-diones in a multi-gram fashion. Treatment of these compounds with a primary amine allows rapid access to various N-substituted indenoisoquinolines, whose in vitro Anticancer activity and Topoisomerase I inhibition have been evaluated.

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