A novel series of carbohydrate-based naphthoquinones was synthesized and evaluated for cytotoxicity against different human cancer cell lines (HCT-116, A-549 and MDA-MB 435). The compounds derived from juglone showed better cytotoxicity profiles.

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Simple methodologies giving access to a new series of pophyrin/4-quinolone conjugates 6 and to the corresponding intracyclized derivatives 8 are described. The key steps to obtain 6 involved palladium-catalyzed amination reactions of 6bromo-4-quinolones containing N-ethyl, N-pentyl and N-ribofuransyl substituents with (2-amino-5,10,15,20tetraphenylporphyrinato)nickel(II) followed by demetallation. Compounds 8 were obtained from compounds 4, the nickel(II) complexes of 6, by an oxidative intracylization approach. The new conjugates were fully characterized and the evaluation of singlet oxygen production showed that these compounds possess good to high capability to generate singlet oxygen. The efficacy of these derivatives to photoinactivate Staphylococcus aureus, a Gram-positive bacteria, was evaluated and the best results were obtained with the N-ethyl derivatives 8a and 6a. Results and discussion Synthesis of porphyrin/4-quinolone conjugatesThe synthetic strategy to obtain the new porphyrin/4quinolone conjugates 6 and 8 involved the experimental work

Quinolones have a large bio-dynamicity. Although they are well known as antibacterials, another important activity has been investigated - quinolones are able to inhibit cancer cell proliferation. In view of the great versatility associated with the synthesis of quinolones, many researchers have spent time and resources on the development of new structurally diversified quinolone derivatives with the purpose of finding new possibilities for cancer treatment. In this review some of the most recent advances in the search for new quinolone anticancer agents are highlighted, with focus on naturally occurring substances, bioactive metal complexes, molecular hybrids, photosensitizers and heterocycle condensed quinolones.