Design, synthesis and anticancer activity evaluation of new heterocyclic derivatives as PARP inhibitors /
Ghada Fathy Hussein Elmasry
Design, synthesis and anticancer activity evaluation of new heterocyclic derivatives as PARP inhibitors / تصميم و تشييد بعض المشتقات الحلقية الغير متجانسة كمضادات للسرطان من خلال تثبيط انزيم بارب Ghada Fathy Hussein Elmasry ; Supervised Samir Mohamed Elmoghazy , Fadi Mohsen Awadallah , Enayat Ebrahim Aly - Cairo : Ghada Fathy Hussein Elmasry , 2019 - 110 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 pyrido[2,3-d]pyridazinone derivatives; VIIIa-g, IXa,b, Xa-d and XIa-g as PARP-1 inhibitors. Molecular modeling techniques were used to support the design. The twenty 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. Computational ADME study was conducted to ensure that the most active compounds have proper pharmacokinetic and drug-likeness properties
Olaparib PARP-1 inhibitors Pyridopyridazinones
Design, synthesis and anticancer activity evaluation of new heterocyclic derivatives as PARP inhibitors / تصميم و تشييد بعض المشتقات الحلقية الغير متجانسة كمضادات للسرطان من خلال تثبيط انزيم بارب Ghada Fathy Hussein Elmasry ; Supervised Samir Mohamed Elmoghazy , Fadi Mohsen Awadallah , Enayat Ebrahim Aly - Cairo : Ghada Fathy Hussein Elmasry , 2019 - 110 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 pyrido[2,3-d]pyridazinone derivatives; VIIIa-g, IXa,b, Xa-d and XIa-g as PARP-1 inhibitors. Molecular modeling techniques were used to support the design. The twenty 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. Computational ADME study was conducted to ensure that the most active compounds have proper pharmacokinetic and drug-likeness properties
Olaparib PARP-1 inhibitors Pyridopyridazinones