Zobrazeno 1 - 10 of 20 pro vyhledávání: '"John N, Philoppes"'
1
Akademický článek
Novel N-methylsulfonyl-indole derivatives: biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced cardio vascular risks
Autor: John N. Philoppes, Mohamed A. Abdelgawad, Mohammed A. S. Abourehab, Mohamed Sebak, Mostafa A. Darwish, Phoebe F. Lamie
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1, Pp 246-266 (2023)
Three novel series of N-methylsulfonylindole derivatives 3a&b, 4a–e, and 5a–e were synthesised. Different biological activities of the synthesised compounds were studied. Antimicrobial activity showed that, compounds 4b, 4e and 5d had selective a
Externí odkaz: https://doaj.org/article/403177a113a1494f953f8b744f29c54a
Zobrazit plný text záznamu
2
Akademický článek
Design and synthesis of new indole drug candidates to treat Alzheimer’s disease and targeting neuro-inflammation using a multi-target-directed ligand (MTDL) strategy
Autor: Phoebe F. Lamie, Maha M. Abdel-Fattah, John N. Philoppes
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 2660-2678 (2022)
A novel series of indole-based compounds was designed, synthesised, and evaluated as anti-Alzheimer’s and anti-neuroinflammatory agents. The designed compounds were in vitro evaluated for their AChE and BuChE inhibitory activities. The obtained res
Externí odkaz: https://doaj.org/article/4fc73e36c7ed42c7938bd974b96b3387
Zobrazit plný text záznamu
3
Akademický článek
2-Thiopyrimidine/chalcone hybrids: design, synthesis, ADMET prediction, and anticancer evaluation as STAT3/STAT5a inhibitors
Autor: Phoebe F. Lamie, John N. Philoppes
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 864-879 (2020)
A novel 2-thiopyrimidine/chalcone hybrid was designed, synthesised, and evaluated for their cytotoxic activities against three different cell lines, K-562, MCF-7, and HT-29. The most active cytotoxic derivatives were 9d, 9f, 9n, and 9p (IC50=0.77–1
Externí odkaz: https://doaj.org/article/5323007f7464438c93435026ff8bb74d
Zobrazit plný text záznamu
5
Akademický článek
Novel tetrazole and cyanamide derivatives as inhibitors of cyclooxygenase-2 enzyme: design, synthesis, anti-inflammatory evaluation, ulcerogenic liability and docking study
Autor: Phoebe F. Lamie, John N. Philoppes, Amany A. Azouz, Nesreen M. Safwat
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 805-820 (2017)
Nineteen new compounds containing tetrazole and/or cyanamide moiety have been designed and synthesised. Their structures were confirmed using spectroscopic methods and elemental analyses. Anti-inflammatory activity for all the synthesised compounds w
Externí odkaz: https://doaj.org/article/950c0a3e47da4edd88afd02c9cafc85d
Zobrazit plný text záznamu
7
Akademický článek
Design, Synthesis and Evaluation of Novel Phthalimide Derivatives as in Vitro Anti-Microbial, Anti-Oxidant and Anti-Inflammatory Agents
Autor: Phoebe F. Lamie, John N. Philoppes, Ahmed O. El-Gendy, Lucie Rarova, Jiri Gruz
Publikováno v: Molecules, Vol 20, Iss 9, Pp 16620-16642 (2015)
Sixteen new phthalimide derivatives were synthesized and evaluated for their in vitro anti-microbial, anti-oxidant and anti-inflammatory activities. The cytotoxicity for all synthesized compounds was also determined in cancer cell lines and in normal
Externí odkaz: https://doaj.org/article/f9e6290f029e4c5f8350b83bfcd65991
Zobrazit plný text záznamu
9
Design, synthesis, and pharmacological evaluation of novel and selective COX-2 inhibitors based on celecoxib scaffold supported with in vivo anti-inflammatory activity, ulcerogenic liability, ADME profiling and docking study
Autor: Khaled R A, Abdellatif, Eman K A, Abdelall, Heba A H, Elshemy, John N, Philoppes, Emad H M, Hassanein, Nesma M, Kahk
Publikováno v: Bioorganic Chemistry. 120:105627
Four new series of 1,2,4 triazole derivatives 4a,b 5a-d, 6a-f, and 7a,b possessing methylsulphonylphenyl moiety as COX-2 pharmacophore were designed and synthesized. The target compounds were prepared and evaluated in-vitro against COX-1 and COX-2 en
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a99ed12e8d00dbc63926aebbb6f96c55
https://doi.org/10.1016/j.bioorg.2022.105627
Zobrazit plný text záznamu
10
Design, synthesis, stereochemical determination, molecular docking study, in silico pre-ADMET prediction and anti-proliferative activities of indole-pyrimidine derivatives as Mcl-1 inhibitors
Autor: Phoebe F. Lamie, John N. Philoppes
Publikováno v: Bioorganic Chemistry. 116:105335
In this study, fourteen novel indole-pyrimidine hybrids were designed and synthesized. Their chemical structures were confirmed using different spectroscopic techniques (1H NMR, 13C NMR, IR and mass). Their (E) stereochemical configuration was determ
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe0cd31ddde3688ffa0ad1709a627459
https://doi.org/10.1016/j.bioorg.2021.105335
Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání

Omezení vyhledávání
Plný text Recenzováno Digitální knihovna AV ČR
Zdroje