Synthesis and Biological Properties of Highly Sequence-Specific-Alkylating N-Methylpyrrole–N-Methylimidazole Polyamide Conjugates

Four new alkylating N-methylpyrrole-N-methylimidazole (PI) polyamide conjugates (1–4) with seven-base-pair (bp) recognition ability were synthesized. Evaluation of their DNA-alkylating activity clearly showed accurate alkylation at match site(s). The cytotoxicities of conjugates 1–4 were determined...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-03, Vol.55 (5), p.2057-2066
Hauptverfasser:	Kashiwazaki, Gengo, Bando, Toshikazu, Yoshidome, Tomofumi, Masui, Seiji, Takagaki, Toshiki, Hashiya, Kaori, Pandian, Ganesh N, Yasuoka, Junichi, Akiyoshi, Kazunari, Sugiyama, Hiroshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents, Alkylating - chemical synthesis Antineoplastic Agents, Alkylating - chemistry Antineoplastic Agents, Alkylating - pharmacology Cell Line, Tumor DNA - chemistry Drug Screening Assays, Antitumor Electrophoresis, Polyacrylamide Gel Gene Expression Profiling Gene Expression Regulation Genome, Human Humans Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Liposomes Male Mice Mice, Nude Neoplasm Transplantation Nylons - chemical synthesis Nylons - chemistry Nylons - pharmacology Oligonucleotide Array Sequence Analysis Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Structure-Activity Relationship Transplantation, Heterologous
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