1. Novel Ag(I)‐based 1,2,4‐Oxadiazole Complexes: Synthesis, X‐Ray Crystal Structure, and Biological Evaluation as Anticancer Candidates.
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Ayoup, Mohammed Salah, Alashhab, Rabia E., Soliman, Saied M., Abdel‐Hamid, Hamida, Cordes, David B., McKay, Aidan P., Ghareeb, Doaa A., Masoud, Aliaa, Kassab, Asmaa E., and Abd Al Moaty, Mohamed N.
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TRYPSIN , *SINGLE crystals , *CRYSTAL structure - Abstract
ABSTRACT The 3,5‐diaryl‐1,2,4‐oxadiazole scaffolds
2 and3 were synthesized and used as ligands to obtain three novel Ag(I) complexes4–6 . The structure of the Ag(I) complexes4–6 has been confirmed by single crystal X‐ray diffraction. Complex4 has the dinuclear formula[Ag(2)(NO 3 )] 2 .5 and6 are monomeric complexes having the formula[Ag(3) 2 (NO 3 )] and[Ag(3) 2 ]ClO 4 , respectively. In vitro, trypsin, ALDH2, and iNOS inhibition activities were assessed for the free ligands and their Ag(I) complexes. Interestingly, Ag(I) complexes4–6 revealed more prominent trypsin inhibitory activity than the ligands2 and3 . The oxadiazole derivative3 and its Ag(I) complex (6 ) showed significant ALDH2 inhibition (45% and 55%, respectively). Complex6 (IC50 = 35.61 μM) surpassed its 1,2,4‐oxadiazole ligand3 (IC50 = 88 μM) and evidenced the most prominent ALDH2 inhibitory activity. The oxadiazole derivative3 and its corresponding Ag(I) complexes5 and6 showed significant iNOS inhibition (77.77%, 84.12%, and 84.15%, respectively). With IC50 values of 18.13, 18.15, and 13.96 μM, respectively, complex6 is the most potent against iNOS, surpassing the reference standard. [ABSTRACT FROM AUTHOR]- Published
- 2024
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