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Acridines

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Ippolito Antonini – One of the best experts on this subject based on the ideXlab platform.

Malcolm F. G. Stevens – One of the best experts on this subject based on the ideXlab platform.

Upendra Sharma – One of the best experts on this subject based on the ideXlab platform.

S Martelli – One of the best experts on this subject based on the ideXlab platform.

  • rational design synthesis and biological evaluation of bis pyrimido 5 6 1 de Acridines and bis pyrazolo 3 4 5 kl acridine 5 carboxamides as new anticancer agents
    Journal of Medicinal Chemistry, 2004
    Co-Authors: Ippolito Antonini, Paolo Polucci, Amelia Magnano, Silvia Sparapani, S Martelli
    Abstract:

    The good results obtained with pyrimido[5,6,1-de]Acridines 7 and with pyrazolo[3,4,5-kl]acridinecarboxamides 8 prompted us to the synthesis of two new series of bis acridine derivatives:  the bis(pyrimidoAcridines) 5 and the bis(pyrazoloacridinecarboxamides) 6. Compounds 5 can be regarded also as cyclized derivatives of bis(acridine-4-carboxamides) 3 and compounds 6 as cyclized derivatives of bis(acridine-4-carboxamides) 4. The noncovalent DNA-binding properties of these compounds have been examined using fluorometric techniques. The results indicate that (i) the target compounds are excellent DNA ligands; (ii) the bis derivatives 5 and 6 are more DNA-affinic than corresponding monomers 7 and 8; (iii) the new bis 5 and 6 result always less efficient in binding than related bis(acridine-4-carboxamides) 3 and 4; and (iv) in both series 5 and 6 a clear, remarkable in some cases, preference for binding to AT rich duplexes can be noted. In vitro cytotoxic potency of these derivatives toward the human colon ade…

William A. Denny – One of the best experts on this subject based on the ideXlab platform.

  • Synthesis and cytotoxicity of potential anticancer derivatives of pyrazolo[3,4,5-kl]acridine and indolo[2,3-a]acridine
    Tetrahedron, 2002
    Co-Authors: Junjie Chen, Leslie W. Deady, William A. Denny
    Abstract:

    Abstract Pyrazolo[3,4,5- kl ]Acridines were prepared by reaction of ethyl 1,9-dioxo-1,2,3,4,9,10-hexahydroacridine-4-carboxylate ( 4 ) with hydrazine and its methyl and 2-(dimethylamino)ethyl derivatives, followed by aromatization of the intermediate products with 1,4-benzoquinone. Conversion of the ester function to a carboxamide was also carried out and N -(2-(dimethylamino)ethyl)-1-(2-(dimethylamino)ethyl)-1,2-dihydropyrazolo[3,4,5- kl ]acridine-5-carboxamide ( 13c ) was appreciably cytotoxic in a panel of cell lines. Reaction of 4 with 4-methoxyphenylhydrazine gave instead a novel indolo[2,3- a ]acridine derivative.

  • The genetic toxicology of Acridines.
    Mutation research, 1991
    Co-Authors: Lynnette R. Ferguson, William A. Denny
    Abstract:

    Acridine and its derivatives are planar polycyclic aromatic molecules which bind tightly but reversibly to DNA by intercalation, but do not usually covalently interact with it. Acridines have a broad spectrum of biological activities, and a number of derivatives are widely used as antibacterial, antiprotozoal and anticancer drugs. Simple Acridines show activity as frameshift mutagens, especially in bacteriophage and bacterial assays, by virtue of their intercalative DNA-binding ability. Acridines bearing additional fused aromatic rings (benzAcridines) show little activity as frameshift mutagens, but interact covalently with DNA following metabolic activation (forming predominantly base-pair substitution mutations). Compounds where the acridine acts as a carrier to target alkylating agents to DNA (e.g. the ICR compounds) cause predominantly frameshift as well as base-pair substitution mutations in both bacterial and mammalian cells. NitroAcridines may act as simple Acridines or (following nitro group reduction) as alkylating agents, depending upon the position of the nitro group. Acridine-based topoisomerase II inhibitors, although frameshift mutagens in bacteria and bacteriophage systems, are primarily chromosomal mutagens in mammalian cells. These mutagenic activities are important, since the compounds have considerable potential as clinical antitumour drugs. Although evidence suggests that simple Acridines are not animal or human carcinogens, a number of the derived compounds are highly active in this capacity.