Browsing by Author "Khalil N.A."

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    Synthesis and cytotoxic activity of certain trisubstituted azetidin-2-one derivatives as a cis-restricted combretastatin A-4 analogues
    (Pharmaceutical Society of Korea, 2017) Elmeligie S.; Taher A.T.; Khalil N.A.; El-said A.H.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); 6th October City; Giza; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Misr University for Science and Technology; 6th October City; Giza; Egypt
    Novel series of 1,3,4-trisubstituted azetidin-2-one derivatives 8a�p were synthesized and proposed as cytotoxic agents acting via inhibition of tubulin at the colchicine binding site. The design of the target compounds was based upon modification in the structure of the vascular targeting agent combretastatin A-4 (CA-4). The cis double bond linker in CA-4 was replaced with the azetidin-2-one ring aiming to prevent the cis/trans isomerization that suppresses the activity of CA-4, thereby enhancing its antiproliferative activity. All new compounds were investigated in vitro against MCF-7 and HCT-116 cell lines. The inhibition of tubulin polymerization by four most potent compounds 8g, 8j, 8n and 8o was also evaluated. The synthesis of the final targets was achieved adopting Staudinger reaction. Molecular modeling studies were performed to rationalize the biological results. � 2016, The Pharmaceutical Society of Korea.
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    Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking
    (Academic Press Inc., 2019) Ahmed E.M.; Khalil N.A.; Taher A.T.; Refaey R.H.; Nissan Y.M.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October 6 University; Giza; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt
    Novel series of some triazolo[4,3-b]pyridazine derivatives were designed and synthesized. All the newly synthesized compounds were evaluated for their cytotoxic activity at 10?5 M concentration towards 60 cancer cell lines according to USA NCI protocol. Most of the synthesized compounds showed good activity against SR (leukemia) cell panel. The most active compounds, 2f and 4a were subjected for further evaluation at a five dose level screening and their efficacy for c-Met kinase inhibition was determined in vitro. Binding mode of these derivatives was explored via molecular docking. 2019 Elsevier Inc.