[HTML][HTML] Vascular endothelial growth factor receptor (VEGFR-2)/KDR inhibitors: medicinal chemistry perspective

SJ Modi, VM Kulkarni - Medicine in Drug Discovery, 2019 - Elsevier
New blood vessels formation from the existing vasculature is called angiogenesis. It is an
essential physiological process for the growth of cells, tissue repair, wound healing, and …

[HTML][HTML] Diarylureas as antitumor agents

A Catalano, D Iacopetta, MS Sinicropi, C Franchini - Applied Sciences, 2021 - mdpi.com
The diarylurea is a scaffold of great importance in medicinal chemistry as it is present in
numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti …

Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors

AE Abdallah, RR Mabrouk, MMS Al Ward… - Journal of Enzyme …, 2022 - Taylor & Francis
Based on quinazoline, quinoxaline, and nitrobenzene scaffolds and on pharmacophoric
features of VEGFR-2 inhibitors, 17 novel compounds were designed and synthesised …

Design, synthesis and evaluation of novel thienopyrimidine-based agents bearing diaryl urea functionality as potential inhibitors of angiogenesis

A Faraji, TO Bakhshaiesh, Z Hasanvand… - European Journal of …, 2021 - Elsevier
Inhibition of angiogenesis is a promising strategy for the treatment of cancer. Herein, we
describe the design and synthesis of thieno [2, 3-d] pyrimidine-1, 3, 4-thiadiazole-aryl urea …

Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase

X Yuan, Q Yang, T Liu, K Li, Y Liu, C Zhu… - European Journal of …, 2019 - Elsevier
Herein, we have carried out a structural optimization campaign to discover the novel anti-
tumor agents with our previously screened YQY-26 as the hit compound. A library of thirty …

Design, synthesis, antitumor, and VEGFR-2 inhibition activities of novel 4-anilino-2-vinyl-quinazolines: Molecular modeling studies

A Hamdi, HW El-Shafey, DIA Othman, AS El-Azab… - Bioorganic …, 2022 - Elsevier
The antitumor activity of newly synthesized 4-anilino-2-vinylquinazolines 8a-r was measured
comparable to sorafenib as a standard drug. The 2-vinylquinazolines 8a-r were evaluated …

Towards multi-target antidiabetic agents: Discovery of biphenyl-benzimidazole conjugates as AMPK activators

DA Babkov, ON Zhukowskaya, AV Borisov… - Bioorganic & medicinal …, 2019 - Elsevier
Type 2 diabetes mellitus is a complex metabolic disorder requiring polypharmacology
approaches for effective treatment. Combinatorial library of fifteen new tricyclic …

Diaryl urea: a privileged structure in anticancer agents

L Garuti, M Roberti, G Bottegoni… - Current medicinal …, 2016 - ingentaconnect.com
The diaryl urea is an important fragment/pharmacophore in constructing anticancer
molecules due to its near-perfect binding with certain acceptors. The urea NH moiety is a …

Oxytrofalcatin Puzzle: Total Synthesis and Structural Revision of Oxytrofalcatins B and C

K Sugitate, T Yamashiro, I Takahashi… - The Journal of …, 2023 - ACS Publications
The previously reported structures of oxytrofalcatins B and C possess a benzoyl indole core.
However, following synthesis and NMR comparison of both the proposed structure and the …

Quinoxalinone (Part II). Discovery of (Z)-3-(2-(pyridin-4-yl) vinyl) quinoxalinone derivates as potent VEGFR-2 kinase inhibitors

L Shi, J Zhou, J Wu, J Cao, Y Shen, H Zhou… - Bioorganic & Medicinal …, 2016 - Elsevier
Inhibition of VEGFR-2 kinase has been highlighted as one of the well-defined strategies to
suppress tumor growth via blockade of angiogenesis. Guided by the principles of …