A series of 13 novel 3-hydroxyindolin-2-one-benzo[4,5]imidazo[2,1-b]thiazole hybrids was designed, synthesized, and evaluated as potential anti-Alzheimer agents targeting monoamine oxidase B (MAO-B) and cholinesterases. The target compounds were obtained by condensing a benzo[4,5]imidazo[2,1-b]thiazole-based ketone wit...
Wagdy M. Eldehna, Ashraf K. El-Damasy, Jaeyeop Lim et al.· RSC Advances· 0 citations
The development of innovative treatment medicines that can overcome drug resistance and intracellular persistence is necessary since tuberculosis (TB) continues to be a significant worldwide health burden. In this work, series of hybrid compounds containing azole moieties, imine/semicarbazide linkers, and isonicotinoyl...
Wagdy M. Eldehna, Zainab M. Elsayed, M. Korycka-Machała et al.· RSC Medicinal Chemistry· 0 citations
A new series of quinazolinone–triazole hybrids (QTHs, 5a–n) was designed, synthesized, and evaluated as potential multi-target-directed ligands for Alzheimer's disease. All synthesized compounds were screened against human monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). The obtained results revealed pronou...
Wagdy M. Eldehna, Ashraf K El-Damasy, Jaeyeop Lim et al.· RSC Advances· 1 citation
The ongoing emergence of SARS-CoV-2 mutations underscores the urgent need for new antivirals that target key viral proteins. This study describes the design, synthesis, and evaluation of two series of 1,3,4-oxadiazole-tethered N-substituted isatin hybrids as inhibitors of the SARS-CoV-2 main protease (Mpro): 1,2,3-tria...
T. Al-Warhi, Md Sofequl Islam Mukim, Zainab M. Elsayed et al.· RSC Advances· 0 citations
A series of alkyl coumarin-tethered phenyl quinazolinones were rationally designed and synthesized as hypoxia-targeted dual hCA IX/HSP90α inhibitors, exhibiting potent, highly selective inhibition of hCA IX (in the nanomolar range), while displaying negligible activity against the off-target isoforms hCA I and II.
Amal S. Elgohary, Mervat H. El-Hamamsy, N. Sharafeldin et al.· RSC Advances· 0 citations
Isocitrate dehydrogenase (IDH) enzymes convert isocitrate to α-ketoglutarate. When IDH1 or IDH2 is mutated, the enzyme gains a new function, and the oncometabolite D-2-hydroxyglutarate (D-2-HG) accumulates. Its epigenetic and metabolic effects depend on the tumor context. This review classifies mutant IDH inhibitors by...
Moataz A. Shaldam, Anwar A. El-Hamaky, Nourhan A. Khattab et al.· Drug Discovery Today· 0 citations
The consistent binding of compound 5 d within the ATP‐binding pocket of CDK‐2 was confirmed by molecular docking and molecular dynamics simulations, and attractive drug‐like and pharmacokinetic features, similar to those of Roscovitine, were demonstrated by in silico ADMET predictions.
Wagdy M. Eldehna, Zainab M. Elsayed, Mohamed R. Elnagar et al.· Drug development research (P...· 0 citations
