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DNA Metalating–Intercalating Hybrid Agents for the Treatment of Chemoresistant Cancers
Author(s) -
Suryadi Jimmy,
Bierbach Ulrich
Publication year - 2012
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201202050
Subject(s) - pharmacophore , cisplatin , acridine , platinum , combinatorial chemistry , dna , chemistry , intercalation (chemistry) , computational biology , pharmacology , cancer research , bioinformatics , medicine , biology , stereochemistry , chemotherapy , biochemistry , organic chemistry , catalysis
Nonclassical platinum‐based antitumor agents have shown enormous potential in the treatment of chemoresistant cancers. The design of these agents is based on the hypothesis that platinum‐containing pharmacophores that react with nuclear DNA in cancer cells radically differently than the clinical agent cisplatin will produce a unique spectrum of biological activity. One such class of molecules are platinum–acridine hybrid agents derived from the prototypical complex [PtCl(en)(ACRAMTU)](NO 3 ) 2 , en=ethane‐1,2‐diamine, ACRAMTU=1‐[2‐(acridin‐9‐ylamino)ethyl]‐1,3‐dimethylthiourea (“PT–ACRAMTU”). This article summarizes milestones in the development of these agents and reviews critical key concepts that have guided their design and that of related compounds.