Design, synthesis and in silico studies of new quinazolinone derivatives as antitumor PARP-1 inhibitors.
Autor: | Ramadan SK; Department of Chemistry, Faculty of Science, Ain Shams University Abbassia 11566 Cairo Egypt elsayedam@sci.asu.edu.eg., Elrazaz EZ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University Abbassia 11566 Cairo Egypt khaled.abouzid@pharma.asu.edu.eg., Abouzid KAM; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University Abbassia 11566 Cairo Egypt khaled.abouzid@pharma.asu.edu.eg.; Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City Sadat City Egypt., El-Naggar AM; Department of Chemistry, Faculty of Science, Ain Shams University Abbassia 11566 Cairo Egypt elsayedam@sci.asu.edu.eg. |
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Jazyk: | angličtina |
Zdroj: | RSC advances [RSC Adv] 2020 Aug 10; Vol. 10 (49), pp. 29475-29492. Date of Electronic Publication: 2020 Aug 10 (Print Publication: 2020). |
DOI: | 10.1039/d0ra05943a |
Abstrakt: | Herein, we report an eco-friendly synthesis of a new series of quinazolinone-based derivatives as potential PARP-1 inhibitors. The 4-quinazolinone scaffold was utilized as a bioisostere to the phthalazinone core of the reference compound Olaparib. Most of the synthesized compounds displayed appreciable inhibitory activity against PARP-1. Compound 12c showed inhibitory activity at IC Competing Interests: The authors declare no conflict of interest, financial or otherwise. (This journal is © The Royal Society of Chemistry.) |
Databáze: | MEDLINE |
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