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Abstract
A series of benzo [d] [1,3] azoles 2-substituted with benzyl- and allyl-sulfanyl groups were synthesized, and their cytotoxic activities were in vitro evaluated against a panel of six human cancer cell lines. The results showed that compounds BTA-1 and BMZ-2 have the best inhibitory effects, compound BMZ-2 being comparable in some cases with the reference drug tamoxifen and exhibiting a low cytotoxic effect against healthy cells. In silico molecular coupling studies at the tamoxifen binding site of ERα and GPER receptors revealed affinity and the possible mode of interaction of both compounds BTA-1 and BMZ-2.
Highlights
The series of 2-substituted benzo [d] [1,3] azoles (BTA-1, BZM-2, BOX-3, BTA-4, been pointed out that the mechanisms of action of these benzo [d] [1,3] azole are different, BZM-5 and BOX-6) were synthesized by a procedure previously reported by our highlighting in an important way the signaling pathways modulated by estrogen receptors (ERs) [41,42,43,44]
Most of the benzo[d]azoles here the synthesis and characterization of a series of benzo [d] [1,3] azoles substituted at heterocycle derivatives were obtained as pure microcrystalline solids in good yields
5, and BOX-6 has been complemented with in silico molecular docking studies, these results suggesting that molecules containing the aromatic vinyl moieties are anchoring better to ERα and G-protein coupled estrogen receptor 1 (GPER) than those including the allylic fragments
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. The structures of benzo [d] [1,3] azoles, such as benzimidazole (BZM), benzothiazole (BTA), and benzoxazole (BOX), are highly valued heterocyclic scaffolds in the design and synthesis of new drugs and bioactive agents These heterocyclic nuclei are privileged pharmacophores that exhibit an inherent affinity for various types of receptors involved in different biological signaling pathways, whose derivatives have shown multiple pharmacological functions, including anti-inflammatory, diuretic, antiviral, anti-insomnia, antiparasitic, anticancer, among others (Scheme 1) [5,6,7,8,9,10,11,12,13,14,15].
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