BIOLOGICAL ACTIVITY OF SYNTHESIZED XANTHONE AND THIOXANTHONE ANALOGS

الموضوعات

طب

الملخص

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.

روابط وملفات

التعريف والنوع

رقم الوثيقة

00efb607-a7fc-48da-91b1-fa7231a23550

رقم العقد

0

نوع الوسائط

Crawler

نوع المحتوى

الرسائل العلمية

صيغة المصدر

رسائل ماجيستير

نوع الملف

pdf text

أسماء الملفات

862552_1.pdf

بيانات النشر

ترجمة العنوان

تقييم الفعالية البيولوجية لمركبات مصنعة لمشتقات زانثون وثيوزانثون

ألقاب المؤلفين

[{"name_ar":"سماح عبد المجيد توفيق عقل ","title_ar":"اعداد","title_en":"Preparation"},{"name_ar":"مراد أبو الحسن","title_ar":"اشراف","title_en":"Supervision"},{"name_ar":"معتصم المصري","title_ar":"اشراف","title_en":"Supervision"}]

اللغة

English

المصدر والدورية

اسم المصدر

BIOLOGICAL ACTIVITY OF SYNTHESIZED XANTHONE AND THIOXANTHONE ANALOGS

المحتوى والصفحات

عدد الصفحات

0

كلمات الباحثين

Xanthone,Thioxanthone,Biological,activity.

إشراف وإعداد

الإشراف

مراد أبو الحسن, معتصم المصري

الإعداد

سماح عبد المجيد توفيق عقل

الاقتباسات الببليوغرافية