Design, synthesis, molecular docking, and anticancer activity of phthalazine derivatives as VEGFR‐2 inhibitors

AGA El‐Helby, RRA Ayyad, H Sakr… - Archiv der …, 2017 - Wiley Online Library
Novel series of phthalazine derivatives 6–11 were designed, synthesized, and evaluated for
their anticancer activity against two human tumor cell lines, HCT‐116 human colon …

Phthalazine‐based VEGFR‐2 inhibitors: Rationale, design, synthesis, in silico, ADMET profile, docking, and anticancer evaluations

F Khedr, MK Ibrahim, IH Eissa… - Archiv der …, 2021 - Wiley Online Library
In the designed compounds, a new linker was inserted in the form of fragments with verified
VEGFR‐2 inhibitory potential, including an α, β‐unsaturated ketonic fragment, pyrazole, and …

Design, synthesis, docking, and anticancer evaluations of phthalazines as VEGFR‐2 inhibitors

K El‐Adl, MK Ibrahim, F Khedr… - Archiv der …, 2022 - Wiley Online Library
Abstract Twenty new N‐substituted‐4‐phenylphthalazin‐1‐amine derivatives were
designed, synthesized, and evaluated for their anticancer activities against HepG2, HCT …

N‐Substituted‐4‐phenylphthalazin‐1‐amine‐derived VEGFR‐2 inhibitors: Design, synthesis, molecular docking, and anticancer evaluation studies

K El‐Adl, MK Ibrahim, F Khedr… - Archiv der …, 2021 - Wiley Online Library
In accordance with the significant impetus of the discovery of potent vascular endothelial
growth factor receptor 2 (VEGFR‐2) inhibitors, herein, we report the design, synthesis, and …

Pyridine‐derived VEGFR‐2 inhibitors: rational design, synthesis, anticancer evaluations, in silico ADMET profile, and molecular docking

NM Saleh, AAH Abdel‐Rahman, AM Omar… - Archiv der …, 2021 - Wiley Online Library
Abstract Novel pyridine‐derived compounds (5–19) were designed and synthesized, and
their anticancer activities were evaluated against HepG2 and MCF‐7 cells, targeting the …

1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: synthesis and in vitro biological evaluation

SM Abou-Seri, WM Eldehna, MM Ali… - European journal of …, 2016 - Elsevier
In our endeavor towards the development of effective VEGFR-2 inhibitors, three novel series
of phthalazine derivatives based on 1-piperazinyl-4-arylphthalazine scaffold were …

Design, synthesis, molecular docking, anticancer evaluations, and in silico pharmacokinetic studies of novel 5‐[(4‐chloro/2, 4‐dichloro) benzylidene] thiazolidine‐2, 4 …

K El‐Adl, AGA El‐Helby, H Sakr, RR Ayyad… - Archiv der …, 2021 - Wiley Online Library
The anticancer activity of novel thiazolidine‐2, 4‐diones was evaluated against HepG2, HCT‐
116, and MCF‐7 cells. MCF‐7 was the most sensitive cell line to the cytotoxicity of the new …

Design, synthesis, molecular docking, and anticancer evaluations of 1‐benzylquinazoline‐2,4(1H,3H)‐dione bearing different moieties as VEGFR‐2 inhibitors

K El‐Adl, AGA El‐Helby, H Sakr… - Archiv der …, 2020 - Wiley Online Library
A novel series of 1‐benzylquinazoline‐2, 4 (1H, 3H)‐dione derivatives, 6a, b to 11a–e, was
designed, synthesized, and evaluated for their anticancer activity against HepG2, HCT‐116 …

Exploration of the VEGFR-2 inhibition activity of phthalazine derivatives: design, synthesis, cytotoxicity, ADMET, molecular docking and dynamic simulation

HH Bayoumi, MK Ibrahim, MA Dahab, F Khedr… - RSC …, 2024 - pubs.rsc.org
Novel phthalazine derivatives were designed, synthesized and evaluated against Hep G2
and MCF-7 as VEGFR-2 inhibitors. In particular, compounds 2g and 4a were found to be the …

Benzoxazole/benzothiazole‐derived VEGFR‐2 inhibitors: design, synthesis, molecular docking, and anticancer evaluations

AGA El‐Helby, H Sakr, IH Eissa… - Archiv der …, 2019 - Wiley Online Library
A novel series of benzoxazole/benzothiazole derivatives 4a–c–11a–e were designed,
synthesized, and evaluated for anticancer activity against HepG2, HCT‐116, and MCF‐7 …