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Design, Synthesis, and Biological Evaluation of Novel Hydroxamic Acid-Based Organoselenium Hybrids.

Jameelah S AlotaibiYasair S S Al-FaiyzSaad Shaaban
Published in: Pharmaceuticals (Basel, Switzerland) (2023)
We report the design and synthesis of novel hydroxamic acid-tethered organoselenium (OSe) hybrids. Their antimicrobial and anticancer activities were assessed against different microbes (e.g., Candida albicans ( C. albicans ), Escherichia coli ( E. coli ), and Staphylococcus aureus ( S. aureus )), as well as liver and breast carcinomas. OSe hybrid 8 showed promising anticancer activity, with IC 50 = 7.57 ± 0.5 µM against HepG2 and IC 50 = 9.86 ± 0.7 µM against MCF-7 cells. Additionally, OSe compounds 8 and 15 exhibited promising antimicrobial activities, particularly against C. albicans (IA% = 91.7 and 83.3) and S. aureus (IA% = 90.5 and 71.4). The minimum inhibitory concentration (MIC) assay confirmed the potential antimicrobial activity of OSe compound 8 . OSe compounds 8 and 16 displayed good antioxidant activities compared to vitamin C in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. These results indicate that hydroxamic acid-based organoselenium hybrids have promising biological activities such as anticancer, antimicrobial, and antioxidant properties, especially compounds 8 , 13 , 15, and 16, which warrant further studies.
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