Distamycin Analogues (distamycin + analogue)

Distribution by Scientific Domains


Selected Abstracts


Synthesis and Biological Evaluation of Distamycin Analogues , New Potential Anticancer Agents

ARCHIV DER PHARMAZIE, Issue 2 2009
Danuta Drozdowska
Abstract Eight of analogues of distamycin, potential minor-groove binders, were synthesized and tested for in-vitro cytotoxicity towards human breast cancer cells MCF-7 and MDA-MB-231. The method of synthesis is simple and convenient. All of the compounds 1,8 showed antiproliferative and cytotoxic effects against both cell lines in the range 3.47 to 12.53 ,M for MDA-MB-231 and 4.35 to 12.66 ,M for MCF-7. All compounds demonstrated activity against DNA topoisomerases I and II at a concentration of 50 ,M. The ethidium bromide assay showed that these compounds bind to plasmid pBR322, yet weaker than distamycin. Further investigations concerning the mechanism of cytotoxicity are now in progress, but the IC50 values suggest that synthetic distamycin analogues with a free amino group, 3,4 and 7,8, can serve as potential carriers of strong acting elements, e. g. alkylating groups. [source]


Electrospray ionization tandem mass spectrometric characteristics and fragmentation mechanisms of distamycin analogues

RAPID COMMUNICATIONS IN MASS SPECTROMETRY, Issue 11 2002
Feili Tang
The electrospray ionization tandem mass spectrometric (ESI-MS/MS) characteristics and fragmentation mechanisms of eight distamycin analogues containing N -methylpyrrole and N -methylimidazole were investigated. The members of two isomeric groups of distamycin analogues with the same elemental composition can be distinguished by MS/MS spectra of protonated molecules and of significant fragment ions. Copyright © 2002 John Wiley & Sons, Ltd. [source]


Synthesis and Biological Evaluation of Distamycin Analogues , New Potential Anticancer Agents

ARCHIV DER PHARMAZIE, Issue 2 2009
Danuta Drozdowska
Abstract Eight of analogues of distamycin, potential minor-groove binders, were synthesized and tested for in-vitro cytotoxicity towards human breast cancer cells MCF-7 and MDA-MB-231. The method of synthesis is simple and convenient. All of the compounds 1,8 showed antiproliferative and cytotoxic effects against both cell lines in the range 3.47 to 12.53 ,M for MDA-MB-231 and 4.35 to 12.66 ,M for MCF-7. All compounds demonstrated activity against DNA topoisomerases I and II at a concentration of 50 ,M. The ethidium bromide assay showed that these compounds bind to plasmid pBR322, yet weaker than distamycin. Further investigations concerning the mechanism of cytotoxicity are now in progress, but the IC50 values suggest that synthetic distamycin analogues with a free amino group, 3,4 and 7,8, can serve as potential carriers of strong acting elements, e. g. alkylating groups. [source]