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The 1,2-naphthoquinone compound was previously considered active against solid tumors. Moreover, glycosidase inhibitors such as 1,2,3-1H triazoles has been pointed out as efficient compounds in anticancer activity studies. Thus, a series of eleven 1,2-naphthoquinones tethered in C2 to 1,2,3-1H-triazoles 9a-k were designed, synthesized and their cytotoxic activity evaluated using HCT-116 (colon adenocarcinoma), MCF-7 (breast adenocarcinoma) and RPE (human nontumor cell line from retinal epithelium). The chemical synthesis was performed from C-3 allylation of lawsone followed by iodocyclization with subsequent nucleophilic displacement with sodium azide and, finally, the 1,3-dipolar cycloaddition catalyzed by Cu(I) with terminal alkynes led to the formation of 1H-1,2,3-Triazol-1-ylmethyl-2,3-dihydronaphtho[1,2-b]furan-4,5-diones in good yields. Compounds containing aromatic group linked to 1,2,3-triazole ring (9c, 9d, 9e, 9i) presented superior cytotoxic activity against cancer cell lines with IC50 in the range of 0.74 to 4.4 µM indicating that the presence of aromatic rings substituents in the 1,2,3-1H-triazole moiety is probably responsible for the improved cytotoxic activity.

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The naphthotriazolyl-4-oxoquinoline derivatives were obtained in good to moderate yields, and one of them, 12c, exhibited strong and selective antitumor properties. The antitumor mechanism involves inhibition of glycolysis, diminished intracellular ATP levels, induction of ROS production and triggering of apoptosis. These effects are all selective for cancer cells, since noncancer cells are unaffected, and these effects can only be attributed to the whole molecule, as different pharmacophoric groups did not reproduce these effects.

Chagas disease, considered by the World Health Organization as a neglected tropical disease, is responsible for the deaths of more than 10,000 people annually. The main drugs used to overcome the disease, Benzonidazole and Nifurtimox, besides being old, have limitations regarding the adverse effects related to the treatment time and consequently their toxicity. Therefore, the need for a new drug to be used against this disease becomes evident. The classes of organoselenium and aromatic heterocycles 1,2,3-triazoles are promising for this issue, profile of both classes for further evaluation against Trypanossoma cruzi, the since both have their known chemistry and antiparasitic activity already described. In this work, the molecular hybridization technique was used in order to combine the individual bioactive protozoan that causes Chagas disease. The methodology used was based on works described in the literature. Initially, benzene azides were synthesized from commercial anilines, while ethynyl(phenyl)selane came from differents aromatic diselenides. With these intermediates, a 1,3-dipolar cycle-addition was performed to obtain the new target molecules 1-phenyl-4-(phenylselanyl)-1H-1,2,3-triazoles with moderate to good yields ranged from 52 to 75%. The characterization of the final molecules is in process and when finished they will be send for evaluation of biological activity. It's possible to conclude that the method used is simple and easy to access, an important factor for potential drugs against neglect diseases. After the assessment of bioactivity, it will be possible to identify the efficiency of these substances, as well as, if necessary, the optimization of their structure.

A Assembleia do Nobel, no Instituto de Karolinska, em 05 de outubro de 2015 anunciou os laureados do Prêmio Nobel de Fisiologia ou Medicina deste mesmo ano. Os ganhadores foram William C. Campbell e Satoshi Omura, em conjunto, e Touyou Tu. Campbell e Omura foram laureados pela descoberta de uma nova droga, a avermectina (1), que co ate a o o er ose egueira dos rios e a filaríase li fáti a, i fe ção ausadora da elefantíase. Já Touyou Tu, recebeu o prêmio pela descoberta da artemisina (2), substância que combate os parasitas causadores da malária.¹

Quinones and organochalcogens are classes of compounds with great biological applicability, such as antioxidant, anticancer, anti-Alzheimer, and antidepressant activities, among others. Thus, the combination of these two classes of compounds is important to obtain new hits with biological activities that are additive or synergistic. Several methodologies for the preparation of this class of hybrid compound have been widely described. Many of the prepared hybrid molecules have shown increased biological activities and, in some cases, to act as two distinct pharmacophores. In this review, methods for the preparation of selenium-quinones, tellurium-quinones and their biological applications are highlighted.

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