title: Synthesis and evaluation of sequence-specific DNA alkylating agents: effect of alkylation subunits.
abstract: We have demonstrated that hairpin pyrrole (Py)- imidazole (Im) polyamide-CBI conjugates selectively alkylate predetermined sequences. In this study, we investigated the effect of alkylation subunits, for example conjugates 1-4 with three types of DNA alkylating units, and Py-Im polyamides with indole linker. Conjugate 3 and 4 selectively alkylated the predetermined sequences as described previously, while conjugates 1 and 2 alkylate at mismatched sites.
authors.affiliation: Department of Chemistry, Graduate School of Science, Kyoto University, Kitashirakawa Oiwakecho, Sakyo-ku, Kyoto 606-8502, Japan.
authors.forename: Tatsuhiko
authors.initials: T
authors.lastname: Shimizu
authors.forename: Shunta
authors.initials: S
authors.lastname: Sasaki
authors.forename: Masafumi
authors.initials: M
authors.lastname: Minoshima
authors.forename: Ken-ichi
authors.initials: K
authors.lastname: Shinohara
authors.forename: Toshikazu
authors.initials: T
authors.lastname: Bando
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Sugiyama
mesh_terms: D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis / Q000737:chemistry*; D020137:Base Pair Mismatch; D001483:Base Sequence; D003521:Cyclopropanes / Q000737:chemistry; D004247:DNA / Q000737:chemistry; D004591:Electrophoresis, Polyacrylamide Gel; D007093:Imidazoles / Q000737:chemistry; D007211:Indoles / Q000737:chemistry; D009757:Nylons / Q000737:chemistry; D011758:Pyrroles / Q000737:chemistry
chemical_list: C506823:1,2,9,9a-tetrahydrocyclopropa(1,2-c)benz(1,2-e)indol-4-one; D018906:Antineoplastic Agents, Alkylating; D003521:Cyclopropanes; D007093:Imidazoles; D007211:Indoles; D009757:Nylons; D011758:Pyrroles; D004247:DNA