Design, synthesis and biological evaluation of some new barbituric acid derivatives with anticipated anticancer activity /
Noura Sayed Hanafy Mahmoud
Design, synthesis and biological evaluation of some new barbituric acid derivatives with anticipated anticancer activity / تصميم: تشييد وتقييم بيولوجى لبعض مشتقات حمض الباربيتيوريك الجديدة ذات نشاط متوقع كمضادات للسرطان Noura Sayed Hanafy Mahmoud ; Supervised Samir Mohamed Elmoghazy , Riham Francois George , Essam Eldin Abdelfattah Osman - Cairo : Noura Sayed Hanafy Mahmoud , 2020 - 100 P. : charts , facsimiles ; 25cm
Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
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
Molecular docking PARP-1 inhibitors Pyrimidinones
Design, synthesis and biological evaluation of some new barbituric acid derivatives with anticipated anticancer activity / تصميم: تشييد وتقييم بيولوجى لبعض مشتقات حمض الباربيتيوريك الجديدة ذات نشاط متوقع كمضادات للسرطان Noura Sayed Hanafy Mahmoud ; Supervised Samir Mohamed Elmoghazy , Riham Francois George , Essam Eldin Abdelfattah Osman - Cairo : Noura Sayed Hanafy Mahmoud , 2020 - 100 P. : charts , facsimiles ; 25cm
Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry
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
Molecular docking PARP-1 inhibitors Pyrimidinones