Recent advances in small organic molecules as DNA intercalating agents: synthesis, activity, and modeling.


:The interaction of small molecules with DNA plays an essential role in many biological processes. As DNA is often the target for majority of anticancer and antibiotic drugs, study about the interaction of drug and DNA has a key role in pharmacology. Moreover, understanding the interactions of small molecules with DNA is of prime significance in the rational design of more powerful and selective anticancer agents. Two of the most important and promising targets in cancer chemotherapy include DNA alkylating agents and DNA intercalators. For these last the DNA recognition is a critical step in their anti-tumor action and the intercalation is not only one kind of the interactions in DNA recognition but also a pivotal step of several clinically used anti-tumor drugs such as anthracyclines, acridines and anthraquinones. To push clinical cancer therapy, the discovery of new DNA intercalators has been considered a practical approach and a number of intercalators have been recently reported. The intercalative binding properties of such molecules can also be harnessed as diagnostic probes for DNA structure in addition to DNA-directed therapeutics. Moreover, the problem of intercalation site formation in the undistorted B-DNA of different length and sequence is matter of tremendous importance in molecular modeling studies and, nowadays, three models of DNA intercalation targets have been proposed that account for the binding features of intercalators. Finally, despite DNA being an important target for several drugs, most of the docking programs are validated only for proteins and their ligands. Therefore, a default protocol to identify DNA binding modes which uses a modified canonical DNA as receptor is needed.


Eur J Med Chem


Rescifina A,Zagni C,Varrica MG,Pistarà V,Corsaro A




Has Abstract


2014-03-03 00:00:00












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    authors: Arafa RK,Nour MS,El-Sayed NA

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    pub_type: 杂志文章,评审


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    pub_type: 杂志文章


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    pub_type: 杂志文章


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    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


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    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


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    pub_type: 杂志文章


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    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


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    更新日期:2017-09-29 00:00:00

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    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Lei S,Zhang D,Qi Y,Chowdhury SR,Sun R,Wang J,Du Y,Fu L,Jiang F

    更新日期:2020-11-01 00:00:00

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    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Salvagnini C,Gharbi S,Boxus T,Marchand-Brynaert J

    更新日期:2007-01-01 00:00:00

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    abstract::A new series of sixteen multifunctional N-benzyl-piperidine-aryl-acylhydrazones hybrid derivatives was synthesized and evaluated for multi-target activities related to Alzheimer's disease (AD). The molecular hybridization approach was based on the combination, in a single molecule, of the pharmacophoric N-benzyl-piper...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Dias Viegas FP,de Freitas Silva M,Divino da Rocha M,Castelli MR,Riquiel MM,Machado RP,Vaz SM,Simões de Lima LM,Mancini KC,Marques de Oliveira PC,Morais ÉP,Gontijo VS,da Silva FMR,D'Alincourt da Fonseca Peçanha D,Castro NG,N

    更新日期:2018-03-10 00:00:00