Jump to main content
Jump to site search

Issue 26, 2012
Previous Article Next Article

Synthesis and evaluation of novel caged DNA alkylating agents bearing 3,4-epoxypiperidine structure

Author affiliations

Abstract

Previously, we reported that the 3,4-epoxypiperidine structure, whose design was based on the active site of DNA alkylating antitumor antibiotics, azinomycins A and B, possesses prominent DNA cleavage activity. In this report, novel caged DNA alkylating agents, which were designed to be activated by UV irradiation, were synthesized by the introduction of four photo-labile protecting groups to a 3,4-epoxypiperidine derivative. The DNA cleavage activity and cytotoxicity of the caged DNA alkylating agents were examined under UV irradiation. Four caged DNA alkylating agents showed various degrees of bioactivity depending on the photosensitivity of the protecting groups.

Graphical abstract: Synthesis and evaluation of novel caged DNA alkylating agents bearing 3,4-epoxypiperidine structure

Back to tab navigation
Please wait while Download options loads

Supplementary files

Publication details

The article was received on 21 Feb 2012, accepted on 30 Apr 2012 and first published on 01 May 2012


Article type: Paper
DOI: 10.1039/C2OB25366F
Citation: Org. Biomol. Chem., 2012,10, 5102-5108
  •   Request permissions

    Synthesis and evaluation of novel caged DNA alkylating agents bearing 3,4-epoxypiperidine structure

    Y. Kawada, T. Kodama, K. Miyashita, T. Imanishi and S. Obika, Org. Biomol. Chem., 2012, 10, 5102
    DOI: 10.1039/C2OB25366F

Search articles by author