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- Title
Synthesis, Characterization, and Preliminary In Vitro Cytotoxic Evaluation of a Series of 2-Substituted Benzo [ d ] [1,3] Azoles.
- Authors
Linares-Anaya, Ozvaldo; Avila-Sorrosa, Alcives; Díaz-Cedillo, Francisco; Gil-Ruiz, Luis Ángel; Correa-Basurto, José; Salazar-Mendoza, Domingo; Orjuela, Adrian L.; Alí-Torres, Jorge; Ramírez-Apan, María Teresa; Morales-Morales, David; Sousa, Maria Emília de; Queiroz, Maria-João R. P.
- 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.
- Subjects
BINDING sites; CELL lines; BREAST cancer; TAMOXIFEN; CANCER cells; AZOLES; BENZOPYRENE
- Publication
Molecules, 2021, Vol 26, Issue 9, p2780
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules26092780