BIOLOGICAL ACTIVITY OF SYNTHESIZED XANTHONE AND THIOXANTHONE ANALOGS
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Date
2022-06-05
Authors
Aqel, Samah
Journal Title
Journal ISSN
Volume Title
Publisher
جامعة النجاح الوطنية
Abstract
Introduction: Xanthone and thioxanthone were used to synthesize a derivative of compounds to test for anticancer, anti-inflammatory, antioxidant and antimicrobial activity. In order to do this, Grignard reagent was added to xanthone and thioxanthone to give a library of tertiary alcohol of phenyl and benzyl xanthone and thioxanthones. After that, some of them were followed by coupling with cysteine to make cysteine analogous. A total of seven compounds were synthesized. The compounds were characterized using the proton and carbon NMR and IR. The synthesized structures were tested for their anticancer, antioxidant, antimicrobial and ant-inflammatory activities.
Results: The test results were promising; compounds Ⅲ showed a very good activity (IC 50= 2.79 µg/ml) against Colon cancer cells (CaCo). While compound 2 showed a good inhibition activity against hepatic HEPG cells (IC 50= 49.2 µg/ml) and compound Ⅰ showed a very good inhibition activity against HeLa cells (IC 50= 60 µg/ml). Compound Ⅳ has a potent antioxidant inhibition activity (IC50= 4.22 µg/ml). Moreover, compound Ⅶ Showed a good anti-inflammatory activity with a COX2 inhibition activity (1.72 µg/ml) and also good selectivity for COX2 (3.81). However, none of the compounds showed antimicrobial activity. The future work requires further an in-vivo testing to understand its pharmacokinetic and pharmacodynamic activity in living system.
Conclusion: Further future work will be carried out to better understand the SAR effects of these compounds.
Description
Introduction: Xanthone and thioxanthone were used to synthesize a derivative of compounds to test for anticancer, anti-inflammatory, antioxidant and antimicrobial activity. In order to do this, Grignard reagent was added to xanthone and thioxanthone to give a library of tertiary alcohol of phenyl and benzyl xanthone and thioxanthones. After that, some of them were followed by coupling with cysteine to make cysteine analogous. A total of seven compounds were synthesized. The compounds were characterized using the proton and carbon NMR and IR. The synthesized structures were tested for their anticancer, antioxidant, antimicrobial and ant-inflammatory activities.
Results: The test results were promising; compounds Ⅲ showed a very good activity (IC 50= 2.79 µg/ml) against Colon cancer cells (CaCo). While compound 2 showed a good inhibition activity against hepatic HEPG cells (IC 50= 49.2 µg/ml) and compound Ⅰ showed a very good inhibition activity against HeLa cells (IC 50= 60 µg/ml). Compound Ⅳ has a potent antioxidant inhibition activity (IC50= 4.22 µg/ml). Moreover, compound Ⅶ Showed a good anti-inflammatory activity with a COX2 inhibition activity (1.72 µg/ml) and also good selectivity for COX2 (3.81). However, none of the compounds showed antimicrobial activity. The future work requires further an in-vivo testing to understand its pharmacokinetic and pharmacodynamic activity in living system.
Conclusion: Further future work will be carried out to better understand the SAR effects of these compounds.
Keywords
Xanthone, Thioxanthone, Biological, activity.