AI Article Synopsis
- A new series of indolin-2-one compounds with an arylidene structure have been developed and tested for their biological activities, focusing particularly on antimicrobial and cytotoxic effects.
- Compounds with a 2-thienyl group showed strong antimicrobial properties, while those with 3-aminophenyl and 2-pyridyl groups displayed superior antifungal activity, particularly against various fungi.
- The compound featuring the 3-aminobenzylidene fragment (4d) demonstrated moderate binding ability to DNA and significantly higher binding to bovine serum albumin (BSA), indicating its potential as a dual-action pharmaceutical candidate for further research in drug discovery.
Article Abstract
Applying a multistep approach, novel indolin-2-ones (IND) that possess an arylidene motif have been synthesized. Eight compounds were chosen for different biological tests (antimicrobial and cytotoxicity). IND containing 2-thienyl (4h) fragment have been found to exhibit good antimicrobial activity against . Molecules that have 3-aminophenyl (4d) or 2-pyridyl (4g) groups have shown the best antifungal activities against all tested fungi. These compounds have also been noticed as promising pharmaceuticals against MCF-7 cancer cell lines. Experimental outcomes from the investigation of the interaction of 4d with DNA implied its moderate binding to DNA ( = 1.35 × 10 and 3.05 × 10 M for EB and Hoechst binder, respectively). However, considerably stronger binding of 4d to BSA has been evidenced ( = 6.1 × 10 M). In summary, IND that contains -aminobenzylidene fragment (4d) exhibits a good dual biological activity making it a promising candidate for further investigation in the drug discovery sector.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10518658 | PMC |
| http://dx.doi.org/10.1039/d3ra04997c | DOI Listing |
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