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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Design, Synthesis and In Vitro Anticancer Activity of a New Class of Bifunctional DNA Intercalators

Author(s): Ana Maria V. Zbancioc, Gheorghita N. Zbancioc, Catalin Tanase, Anca Miron, Cornelia Ursu and Ionel I. Mangalagiu

Volume 7, Issue 9, 2010

Page: [644 - 649] Pages: 6

DOI: 10.2174/157018010792929504

Price: $65


The emphasis of this work was to design and synthetize a new class of bifunctional DNA intercalators, containing in the same molecule an alkylating part and a nitrogen heterocycles intercalator unit. The adopted strategy is general, straightforward, and only involves two steps: acylation and quaternization. An alternative, fast, general, and environmentally friendly method for preparation of these compounds under microwave (MW) irradiation is also presented. The structure of compounds was proven by elemental (C, H, N) and spectral analysis (IR, 1H NMR, 13C NMR, COSY, HMQC, HMBC). The obtained compounds proved to have excellent anticancer activity in vitro. Possible mechanisms of action and structure-activity relationships are discussed.

Keywords: Bifunctional DNA intercalators, Diazine, 1,3-Diazols, Design, Synthesis, Microwave, Anticancer activity, Bifunctional DNA, Nitrogen heterocytes intercalator unit, Microway (M/W), Spectral analysis IR, Structure activity relationships, Cancer therapy, Chemotherapy, Cytotoxicity, Multidrug resistance, DNA-directed alkylating agents, DNA-affinic carriers, Shimadzu GCMS-QP2010, Chemical ionization (CI), CEM corporation, HeLa cell line, Cervicalendothelial carcinoma, DMEM medium, Student's “t” test, Nitrogen mustards, Halo-alkyl-ester chains, Enzyme inhibition, Diazine moieties, Imidazole, Carbamate prodrugs, Topoisomerase inhibitors, Microwave-assisted synthesis, Chromophore, Naphthyridine

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