Investigating the possible mechanisms of pirfenidone to be targeted as a promising anti-inflammatory, anti-fibrotic, anti-oxidant, anti-apoptotic, anti-tumor, and/or anti …
Pirfenidone (PFD) is a non-peptide synthetic chemical that inhibits the production of
transforming growth factor-beta 1 (TGF-β1), tumor necrosis factor-alpha (TNF-α), platelet …
transforming growth factor-beta 1 (TGF-β1), tumor necrosis factor-alpha (TNF-α), platelet …
Ligand-based design on the dog-bone-shaped BIBR1532 pharmacophoric features and synthesis of novel analogues as promising telomerase inhibitors with in vitro …
Telomerase is an outstanding biological target for cancer treatment. BIBR1532 is a non-
nucleoside selective telomerase inhibitor; however, it experiences ineligible …
nucleoside selective telomerase inhibitor; however, it experiences ineligible …
[HTML][HTML] Synthesis of new organoselenium-based succinanilic and maleanilic derivatives and in silico studies as possible SARS-CoV-2 main protease inhibitors
Herein we report the synthesis of organic selenide-based maleanilic and succinanilic acids
in good yields (up to 95%). Their structural identities were elucidated by spectroscopic …
in good yields (up to 95%). Their structural identities were elucidated by spectroscopic …
Lead optimization of BIBR1591 to improve its telomerase inhibitory activity: design and synthesis of novel four chemical series with in silico, in vitro, and in vivo …
AA Al-Karmalawy, MHA Mousa… - Journal of Medicinal …, 2023 - ACS Publications
Herein, modifications to the previously reported BIBR1591 were conducted to obtain
bioisosteric candidates with improved activities. The% inhibition of the newly afforded …
bioisosteric candidates with improved activities. The% inhibition of the newly afforded …
Design and synthesis of novel benzoazoninone derivatives as potential CBSIs and apoptotic inducers: in vitro, in vivo, molecular docking, molecular dynamics, and …
Apparently, tubulin inhibitors binding to the colchicine-binding site (CBS) currently have
outstanding attention for cancer treatment. So, a series of benzo [b] azonin-2-one derivatives …
outstanding attention for cancer treatment. So, a series of benzo [b] azonin-2-one derivatives …
[HTML][HTML] Phenylpyrazolone-1, 2, 3-triazole hybrids as potent antiviral agents with promising SARS-CoV-2 main protease inhibition potential
COVID-19 infection is now considered one of the leading causes of human death. As an
attempt towards the discovery of novel medications for the COVID-19 pandemic, nineteen …
attempt towards the discovery of novel medications for the COVID-19 pandemic, nineteen …
Ligand-based design, synthesis, computational insights, and in vitro studies of novel N-(5-Nitrothiazol-2-yl)-carboxamido derivatives as potent inhibitors of SARS …
The global outbreak of the COVID-19 pandemic provokes scientists to make a prompt
development of new effective therapeutic interventions for the battle against SARS-CoV-2. A …
development of new effective therapeutic interventions for the battle against SARS-CoV-2. A …
The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico …
Abstract Treatment options for the management of breast cancer are still inadequate. This
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …
The effect of novel synthetic semicarbazone-and thiosemicarbazone-linked 1, 2, 3-triazoles on the apoptotic markers, VEGFR-2, and cell cycle of myeloid leukemia
Abstract Vascular Endothelial Growth Factor II (VEGFR-2) has been proved as a rational
target in cancer therapy. Although currently prescribed VEGFR-2 inhibitors are showing …
target in cancer therapy. Although currently prescribed VEGFR-2 inhibitors are showing …
Design and synthesis of novel rigid dibenzo[b,f]azepines through ring closure technique as promising anticancer candidates against leukaemia and acting as …
MF El-Behairy, WH Abd-Allah, MM Khalifa… - Journal of Enzyme …, 2023 - Taylor & Francis
In this research, two novel series of dibenzo [b, f] azepines (14 candidates) were designed
and synthesised based on the rigidification principle and following the reported …
and synthesised based on the rigidification principle and following the reported …