Unknown

Dataset Information

0

Naturally based pyrazoline derivatives as aminopeptidase N, VEGFR2 and MMP9 inhibitors: design, synthesis and molecular modeling.

ABSTRACT: Aminopeptidase N (APN) is regarded as an attractive target for cancer treatment due to its overexpression in various types of malignancies and its close association with cancer angiogenesis, metastasis and invasion. Herein the authors describe the design, synthesis and biological evaluation of some naturally based pyrazoline derivatives. Among these compounds, the diphenylpyrazole carbothioamide 8 showed significant activity and selectivity index (SI = 4.7) on breast (MCF-7) human cancer cell line and was capable of inhibiting APN with pIC50 value of 4.8, comparable to the reference standard. Further evaluation of derivative 8 against VEGFR2 and MMP9 as biomarkers for angiogenesis and invasion showed that the selected compound had an inhibitory activity on both proteins with pIC50 values of 6.7 and 6.4, respectively. Additionally, the migration ability of cells following treatment with the diphenylpyrazole derivative decreased to record a percentage wound closure of 57.77 for compound 8versus 97.03 for the control. The promising derivative arrested cell growth at the G1 phase inducing early and late apoptosis. Finally, docking and ADMET in silico studies were performed.

SUBMITTER: Batran RZ 

PROVIDER: S-EPMC11248911 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Naturally based pyrazoline derivatives as aminopeptidase N, VEGFR2 and MMP9 inhibitors: design, synthesis and molecular modeling.

Batran Rasha Z RZ   Ahmed Eman Y EY   Awad Hanem M HM   Abdel Latif Nehad A NA  

RSC advances 20240715 31

Aminopeptidase N (APN) is regarded as an attractive target for cancer treatment due to its overexpression in various types of malignancies and its close association with cancer angiogenesis, metastasis and invasion. Herein the authors describe the design, synthesis and biological evaluation of some naturally based pyrazoline derivatives. Among these compounds, the diphenylpyrazole carbothioamide 8 showed significant activity and selectivity index (SI = 4.7) on breast (MCF-7) human cancer cell li  ...[more]

Similar Datasets

Unknown Development of pyrazoline-based derivatives as aminopeptidase N inhibitors to overcome cancer invasion and metastasis.
| S-EPMC9034162 | biostudies-literature
Unknown Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors.
| S-EPMC7172530 | biostudies-literature
Unknown New Thiazolyl-Pyrazoline Derivatives as Potential Dual EGFR/HER2 Inhibitors: Design, Synthesis, Anticancer Activity Evaluation and In Silico Study.
| S-EPMC10647861 | biostudies-literature
Unknown Design, synthesis, and biological investigations of new pyrazole derivatives as VEGFR2/CDK-2 inhibitors targeting liver cancer.
| S-EPMC11520136 | biostudies-literature
Unknown Rational Design and Synthesis of a Novel Series of Thiosemicarbazone-Containing Quinazoline Derivatives as Potential VEGFR2 Inhibitors.
| S-EPMC11860020 | biostudies-literature
Unknown Design, Synthesis, Antiproliferative Actions, and DFT Studies of New Bis-Pyrazoline Derivatives as Dual EGFR/BRAF<sup>V600E</sup> Inhibitors.
| S-EPMC10218941 | biostudies-literature
Unknown New β-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.
| S-EPMC9491354 | biostudies-literature
Unknown Pyrrolyl Pyrazoline Carbaldehydes as Enoyl-ACP Reductase Inhibitors: Design, Synthesis and Antitubercular Activity.
| S-EPMC5676022 | biostudies-literature
Unknown Design, Synthesis, Biological Evaluation, and Molecular Modeling of 2-Difluoromethylbenzimidazole Derivatives as Potential PI3Kα Inhibitors.
| S-EPMC8777764 | biostudies-literature
Unknown Design and synthesis of naturally-inspired SARS-CoV-2 inhibitors.
| S-EPMC10034039 | biostudies-literature