Dicationic bis (9-methylphenazine-1-carboxamides): relationships between biological activity and linker chain structure for a series of potent topoisomerase targeted …

…, AJ Stewart, P Charlton, BC Baguley…

Index: Gamage; Spicer; Finlay; Stewart; Charlton; Baguley; Denny Journal of Medicinal Chemistry, 2001 , vol. 44, # 9 p. 1407 - 1415

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Citation Number: 75

Abstract

Bis (9-methylphenazine-1-carboxamides) joined by a variety of dicationic (CH2) n NR (CH2) m NR (CH2) n linkers of varying length (carboxamide NN distances from 11.0 to 18.4 Å) and rigidity were prepared by reaction of 9-methylphenazine-1-carboxylic acid imidazolide with the appropriate polyamines. The compounds were evaluated for growth inhibitory properties in P388 leukemia, Lewis lung carcinoma, and wild-type (JLC) and mutant (JLA and JLD) ...