Browsing by Author "Nissan Y.M."

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Design and synthesis of new quinoxaline derivatives as anticancer agents and apoptotic inducers
(MDPI AG, 2019) El Newahie A.M.S.; Nissan Y.M.; Ismail N.S.M.; Abou El Ella D.A.; Khojah S.M.; Abouzid K.A.M.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Science and Arts (MSA); Cairo; 12611; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Science and Arts (MSA); Cairo; 12611; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmaceutical Sciences and Pharmaceutical Industries; Future University in Egypt; Cairo; 12311; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy Ain Shams University; Abbassia; Cairo 11566; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Nahda University; Beni Suef; 62513; Egypt; Biochemistry Department; Faculty of Science; King Abdulaziz University; Jeddah; 21589; Saudi Arabia; Department of Organic and Medicinal Chemistry; Faculty of Pharmacy; University of Sadat City; Menoufia; 32897; Egypt
The quinoxaline scaffold is a promising platform for the discovery of active chemotherapeutic agents. Three series of quinoxaline derivatives were synthesized and biologically evaluated against three tumor cell lines (HCT116 human colon carcinoma, HepG2, liver hepatocellular carcinoma and MCF-7, human breast adenocarcinoma cell line), in addition to VEGFR-2 enzyme inhibition activity. Compounds VIId, VIIIa, VIIIc, VIIIe and XVa exhibited promising activity against the tested cell lines and weak activity against VEGFR-2. Compound VIIIc induced a significant disruption in the cell cycle profile and cell cycle arrest at the G2/M phase boundary. In further assays, the cytotoxic effect of the highly active compounds was determined using a normal Caucasian fibroblast-like fetal lung cell line (WI-38). Compound VIIIc could be considered as a lead compound that merits further optimization and development as an anti-cancer and an apoptotic inducing candidate against the HCT116 cell line. � 2019 by the authors.
Design, synthesis and biological evaluation of some novel sulfonamide derivatives as apoptosis inducers
(Elsevier Masson SAS, 2017) Mohamed K.O.; Nissan Y.M.; El-Malah A.A.; Ahmed W.A.; Ibrahim D.M.; Sakr T.M.; Motaleb M.A.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; National Cancer Institute; Cancer Biology Department; Cairo University; Egypt; Faculty of Science; Cairo University; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt
Several novel thiazolidinone and fused thiazolidinone derivatives bearing benzenesulfonamide moiety were synthesized and confirmed via spectral and elemental analyses. The newly synthesized compounds were evaluated for their cytotoxic activity on colorectal cancer cell line (Caco-2). All the synthesized compounds showed better activity than the reference standards (Doxorubicin and 5-FU). Investigation of the apoptotic activity of the most active compounds revealed that compounds 3a, 5a, 5c and 6c activate both caspase-3 and Fas-ligand in Caco-2�cell line. Compound 3a was the most active compound with caspase-3 concentration of 0.43�nmol/mL and Fas-ligand concentration of 775.2�pg/mL in treated Caco-2�cells. Compound 3a was radiolabeled with 99mTc and its biodistribution pattern was evaluated in�vivo using normal Swiss Albino mice. 99mTc-compound 3a complex didn't exhibit any accumulation in any body organs except for its accumulation in the colon; target organ; where it showed 8.97��1.35 %ID/g at 15min p. i. that elevated till 16.02��2.43 %ID/g at 120min p. i. � 2017 Elsevier Masson SAS
Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives
(Elsevier Masson SAS, 2019) Mahmoud W.R.; Nissan Y.M.; Elsawah M.M.; Refaey R.H.; Ragab M.F.; Amin K.M.; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; Drug Research Center; Cairo; Egypt; Pharmacology and Toxicology Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt
Twenty four 6-aminocoumarin based derivatives were synthesized according to two schemes. All the compounds were screened for their acetylcholinesterase inhibitory activity where compound 5b proved to be the most potent AChE inhibitor with (IC50 = 37 nM) compared to tacrine and donepezil (IC50 = 55.0 and 59.0 nM, respectively). Six compounds 2f, 2g, 4b, 5b, 8b and 9b revealed superior activity over donepezil and a conclusive structure activity relationship study was conducted explaining the obtained results. Furthermore, compounds 2f, 4b and 5b were investigated for their neurobehavioral effect in vivo. All the tested compounds showed improvement of neurobehavioral experiments using donepezil as reference drug. In addition, compounds 2f, 4b and 5b were able to reduce extracellular deposition of amyloid beta 42 in a comparable manner to donepezil. The binding modes of the synthesized compounds were evaluated in silico via molecular docking in the active site of AChE, as well as molecular dynamics simulation study. A pharmacophore model was generated for the newly synthesized compounds. � 2019 Elsevier Masson SAS
New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES
(Elsevier Masson SAS, 2019) Hassan G.S.; Abdel Rahman D.E.; Abdelmajeed E.A.; Refaey R.H.; Alaraby Salem M.; Nissan Y.M.; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Badr University in Cairo; Badr City; Cairo; 11829; Egypt; National Cancer Institute; Cairo University; FomElkhalig; Kasr Elaini St.; Cairo; 11796; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt
New pyrazole derivatives 2�5 were synthesized and evaluated for their COX-1 and COX-2 inhibitory activity in vitro. All compounds showed good inhibitory activity at a nanomolar level and most compounds exhibited selectivity towards COX-2 inhibition. Compounds 2a, 3b, 4a, 5b and 5e exhibited IC50 towards COX-2 enzyme of 19.87, 39.43, 61.24, 38.73 and 39.14 nM, respectively. Furthermore, compounds 3b, 4a, 5b and 5e exhibited a selectivity index of 22.21, 14.35, 17.47 and 13.10, respectively. The most active compounds were further subjected to in vivo anti-inflammatory assay. The tested compounds showed better or comparable activity to celecoxib as positive control. In order to explore their binding mode and selectivity behaviour, molecular docking in the active site of COX-2 was carried out for these derivatives. Analysis of the docked poses of the compounds showed that they adopt similar conformations to the highly selective COX-2 inhibitor, SC-558. The docking pose of compound 3b was confirmed by molecular dynamics. All the tested compounds exhibited potent inhibitory effect on the production of PGE2, in addition to their inhibition of COX-2 enzyme. � 2019 Elsevier Masson SAS
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.