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Synthetic analogues of netropsin and distamycin. V. Synthesis of a carbocyclic bis-lexitropsin as potential DNA cleaving agent.

A carbocyclic analogue of bis-distamycin, in which N-methylpyrroles were replaced by two trisubstituted benzene moieties joined by tetramethylenedioxy linkage, has been prepared. This compound bearing photosensitive benzotriazole moieties at the N-terminal residues. The synthetic method for the preparation of the bis-benzotriazolyllexitropsin was accomplished in twelve steps starting from 2-hydroxy-5-phenylazobenzoic acid.

Antineoplastic Agents↗

Synthetic analogues of netropsin and distamycin. VI. Synthesis of carbocyclic lexitropsins containing a bioreductive element.

Carbocyclic derivatives of lexitropsines containing of two aromatic rings, N-dimethylaminopropyl group lonked to carboxyl terminus and 5-[bis(2-chloroethyl)-amino]-2,4-dinitrobenzamide group linked to the amino terminus group were synthesed. The N-terminal group should present selective alkylating activity on the DNA of cancer cells in conditions of hypoxia.

Alkylation↗