Design, synthesis, in vitro anti-cancer activity, ADMET profile and molecular docking of novel triazolo [3, 4-a] phthalazine derivatives targeting VEGFR-2 enzyme

AGA El-Helby, H Sakr, RRA Ayyad… - Anti-Cancer Agents …, 2018 - ingentaconnect.com
Background: Extensive studies were reported in the synthesis of several phthalazine
derivatives as promising anticancer agents as potent VEGFR-2 inhibitors. Vatalanib …

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 …

Design, synthesis, molecular docking and anticancer evaluations of 5-benzylidenethiazolidine-2, 4-dione derivatives targeting VEGFR-2 enzyme

K El-Adl, AGA El-Helby, H Sakr, IH Eissa… - Bioorganic …, 2020 - Elsevier
Abstract Novel series of 5-benzylidenethiazolidine-2, 4-dione derivatives 4 ac-8 af were
designed, synthesized and evaluated for anticancer activity against HepG2, HCT-116 and …

Design, synthesis, in silico and antiproliferative evaluation of novel pyrazole derivatives as VEGFR‐2 inhibitors

P Ravula, HB Vamaraju, M Paturi… - Archiv der …, 2018 - Wiley Online Library
As the blockade of the VEGFR‐2 signaling pathway is a viable approach in cancer therapy,
the present study focuses on a series of pyrazole based VEGFR‐2 inhibitors that were …

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 and molecular docking of new [1, 2, 4] triazolo [4, 3-a] quinoxaline derivatives as anticancer agents targeting VEGFR-2 kinase

NA Alsaif, A Elwan, MM Alanazi, AJ Obaidullah… - Molecular Diversity, 2022 - Springer
Vascular endothelial growth factor receptor-2 (VEGFR-2) is critically involved in cancer
angiogenesis. Blocking of VEGFR-2 signaling pathway proved effective suppression of …

Design and synthesis of phthalazine-based compounds as potent anticancer agents with potential antiangiogenic activity via VEGFR-2 inhibition

S Elmeligie, AM Aboul-Magd, DS Lasheen… - Journal of Enzyme …, 2019 - Taylor & Francis
In the designed compounds, either a biarylamide or biarylurea moiety or an N-substituted
piperazine motif was linked to position 1 of the phthalazine core. The anti-proliferative …

Design, synthesis and molecular modeling study of certain VEGFR-2 inhibitors based on thienopyrimidne scaffold as cancer targeting agents

A Ghith, KM Youssef, NSM Ismail, KAM Abouzid - Bioorganic Chemistry, 2019 - Elsevier
Different series of novel thieno [2, 3-d] pyrimidine derivative (9a-d, 10a-f, l, m and 15a-m)
were designed, synthesized and evaluated for their ability to in vitro inhibit VEGFR-2 …

Synthesis, in vitro anticancer activity and in silico studies of certain isoxazole-based carboxamides, ureates, and hydrazones as potential inhibitors of VEGFR2

SM Abou-Seri, AAM Eissa, MGM Behery, FA Omar - Bioorganic Chemistry, 2021 - Elsevier
The ensuing research presents the results of in vitro anticancer activity of novel 28
compounds of isoxazole–based carboxamides 3 (ad); ureates 4 (ag), 5, 6, 7a, b, 8; and …