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DNA Minor-Groove Binders: Results and Design of New Antitumor Agents

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Sun, 2015-05-24 13:07 — Abdel Naser Zaid
Journal Title, Volume, Page: 
FARMACO Volume: 54 Issue: 1-2 Pages: 15-25 Published: JAN-FEB 1999
Year of Publication: 
1999
Link: 
http://www.sciencedirect.com/science/article/pii/S0014827X98001025
Authors: 
Pier Giovanni Baraldi
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara 17–19, I-44100 Ferrara, Italy
Barbara Cacciari
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara 17–19, I-44100 Ferrara, Italy
Andrea Guiotto
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara 17–19, I-44100 Ferrara, Italy
Romeo Romagnoli
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara 17–19, I-44100 Ferrara, Italy
Abdel Naser Zaid
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara 17–19, I-44100 Ferrara, Italy
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine & Health Sciences, An-Najah National University, Nablus, Palestine
[email protected]
Giampiero Spalluto
Dipartimento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara 17–19, I-44100 Ferrara, Italy
Preferred Abstract (Original): 

DNA minor-groove binding drugs have been extensively studied in the last years in order to influence the regulation of gene expression in neoplastic disorders by means of specific interactions with DNA bases. Pyrrolo[2,1-c][1,4]benzodiazepines (PBDs), CC-1065 and distamycins are three classes of minor-groove alkylating agents which showed interesting cytotoxicity profiles, but they cannot be used in humans for various toxicity problems. For this reason many groups applied heterocyclic substitutions extensively, in order to either modify the reactivity profile or introduce extra interactions within the minor groove, thus changing the binding site or modulating the binding sequence. (C) 1999 Elsevier Science S.A. All rights reserved.