3185-95-3Relevant articles and documents
Design, synthesis, DNA-binding and cytotoxicity evaluation of new potential combilexines
Hotzel, Christian,Marotto, Annalisa,Pindur, Ulf
, p. 367 - 378 (2007/10/03)
Combilexines, compounds in which a DNA intercalator is linked to a minor groove binding component, interact with the DNA in a sequence specific manner to yield in most cases compounds with anticancer activity. A series of new compounds closely related to netropsin in which the two components were linked by an amide group was synthesised as potential combilexines. As some of these compounds showed cytotoxic activity in vitro, an attempt was made to rationalise their mechanism of action. The DNA binding characteristics of the carboxamides were evaluated by thermal denaturation experiments and by ethidium bromide displacement assay. Their ability to inhibit the topoisomerase I was also determined. It was concluded that the new compounds were only weak DNA ligands although able in some cases to inhibit topoisomerase I.
The Synthesis of Radiosensitizers Designed to Bind to the Minor Groove of Duplex DNA
Parrick, John,Porssa, Manuchehr,Jenkins, Terence C.
, p. 2681 - 2686 (2007/10/02)
The synthesis is described of novel compounds, 17, 21, 25 and 27, containing in their molecular architecture both a terminal nitroarene component and an oligopeptide similar to that in the antibiotic distamycin, which is known to bind into the minor groov
Efficient synthesis of oligo-N-methylpyrrolecarboxamides and related compounds
Nishiwaki, Eiji,Tanaka, Shigeaki,Lee, Hideaki,Shibuya, Masayuki
, p. 1945 - 1952 (2007/10/02)
1-Methyl-4-nitro-2-trichloroacetylpyrrole 5, a new precursor for the syntheses of oligo-N-methylpyrrolecarboxamide antibiotics and their analogues, was prepared with facility. The versatility of 5 was demonstrated by the syntheses of oligopeptides 16-19.
