Design, synthesis, and evaluation of mixed imine–amine pyrrolobenzodiazepine dimers with efficient DNA binding affinity and potent cytotoxicity

…, G Ramesh, O Srinivas, P Ramulu, N Laxman…

Index: Kamal, Ahmed; Ramesh; Srinivas; Ramulu; Laxman; Rehana, Tasneem; Deepak; Achary; Nagarajaram Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 20 p. 5427 - 5436

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Citation Number: 12

Abstract

Synthesis of mixed imine–amine pyrrolobenzodiazepine (PBD) dimers that are comprised of DC-81 and secondary amine (N10) of DC-81 subunits tethered to their C8 positions through alkanedioxy linkers (comprised of three and five carbons) is described. These noncross- linking unsymmetrical molecules exhibit significant DNA minor groove binding ability and one of them 5b linked through the pentanedioxy chain exhibits efficient DNA binding ...