SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES OF EXPECTED ANTICANCER ACTIVITY | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Article 5, Volume 64, Issue 2, September and October 2021, Pages 80-92 PDF (852.75 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ajps.2021.187757 | ||
| Author | ||
| Mohamed Alswah | ||
| Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt | ||
| Abstract | ||
| A series of novel pyrazolo[3,4-d]pyrimidine derivatives have designed and synthesized in synthetically useful yields. All the new synthesized compounds were biologically evaluated in vitro for their cytotoxic activities against a panel of three cancer cell lines namely, HepG-2, MCF-7, and HCT-116. The results of cytotoxic evaluation indicated that compound (9) exhibited the most prominent cytotoxic effect against all tested cell lines with IC50 values ranging from (4.03- 6.18) µM comparable to that of doxorubicin as a control drug (IC50 values of 8.17 and 9.27 µM). In particular, compounds (8,9,11) and (12) exhibited higher intercalative activity with IC50 value of 30 µM than doxorubicin (31 µM). | ||
| Keywords | ||
| Anticancer; pyrazolopyramidine derivatives; Topoisomerase II; DNA-intercalator | ||
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