Iso-cbi and iso-ci analogs of cc-1065 and the duocarmycins

Details Iso-cbi and iso-ci analogs of cc-1065 and the duocarmycins Iso-cbi and iso-ci analogs of cc-1065 and the duocarmycins

C - Chemistry, Metallurgy

07

D

C07D 209/04 (2006.01) C07D 209/12 (2006.01) C07D 209/42 (2006.01) C07D 209/56 (2006.01) C07D 209/60 (2006.01) C07D 209/80 (2006.01) C07D 209/90 (2006.01) C07D 209/94 (2006.01) C07D 403/06 (2006.01) C07D 403/14 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2306420

A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhance reactivity.

L'invention porte sur la synthèse d'une série d'analogues bioactifs du (+)-CC-1065 (1) et sur les duocarmycines 2 et 3. Les analogues bioactifs comprennent soit l'iso-CI ou l'iso-CBI (6 et 7) en tant que sous-unités d'alkylation de l'ADN. Différentes sous-unités de fixation de l'ADN sont conjuguées aux sous-unités d'alkylation de l'ADN. Les analogues bioactifs conservent leur sélectivité vis à vis de l'ADN et présentent une réactivité améliorée.

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