الفهرس | Only 14 pages are availabe for public view |
Abstract This work deals with the design and synthesis of some novel pyrimidinone derivatives; Va-e, VIa-e, VIIa-e, Xa-d, XIa-d and XIIa-d as PARP-1 inhibitors. Molecular modeling techniques were used to support the design.The twenty seven newly synthesized compounds were evaluated for their ability to inhibit PARP-1.The in vitro cytotoxic activity of the target compounds was also performed at National Cancer Institute, NCI, Maryland, USA against sixty cell lines.The most active compounds against PARP1 in vitro were evaluated in the BRCA1 mutated breast cancer cell line MDA-MB-436 |