Synthesis and evaluation of N -(benzofuran-5-yl)aromaticsulfonamide derivatives as novel HIF-1 inhibitors that possess anti-angiogenic potential

Wei, Jinlian; Yang, Yingrui; Li, Yali; Mo, Xiaofei; Guo, Xiaoke; Zhang, Xiaojin; Xu, Xiu; Jiang, Zhengyu; Qin, You

doi:10.1016/j.bmc.2016.06.021

Cited by 16 publications

(38 citation statements)

References 36 publications

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“…However, the hemocytometer is time-consuming, more prone to sampling error, and can only measure the high density of cells; therefore, other fluorescence-based kits (e.g., CyQuant) and automated platforms such as plate cytometers can be used instead for analyzing cell proliferation [8]. Other methods have also been developed to circumvent the tediousness of counting cells, including colorimetric assays and DNA synthesis assays [10,11,12,13], described next.…”

Section: In Vitro Assaysmentioning

confidence: 99%

“…The most commonly used colorimetric assay utilizes the biomolecule 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, known as MTT, which is metabolized by mitochondria in living cells; this means that a larger cell population will reduce MTT faster [14]. MTT in particular is widely used in colorimetric assays because it is yellow before it is broken down into a purple formazan [12,13]. The formazan dye produced by the ECs is dissolved in a solvent system that is then tested for absorbance with a spectrophotometer [10].…”

Section: In Vitro Assaysmentioning

confidence: 99%

“…The formazan dye produced by the ECs is dissolved in a solvent system that is then tested for absorbance with a spectrophotometer [10]. Recently, MTT assay results showed that a potential hypoxia-inducible factor-1 (HIF-1) inhibitor that limits angiogenesis did not disrupt living ECs [12], while other MTT assay results elucidated the strong anti-angiogenic properties of certain thiabendazole derivatives on multiple ECs [13].…”

Section: In Vitro Assaysmentioning

confidence: 99%

“…This assay is relatively simple compared to other migration-based assays, but achieving reproducibility proves difficult nonetheless. The issues with reproducibility arise from inconsistencies in confluency as well as data that can be inherently difficult to measure accurately [10,12].…”

Section: In Vitro Assaysmentioning

confidence: 99%

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Evaluation of Angiogenesis Assays

Stryker¹,

Rajabi

Davis

et al. 2019

Biomedicines

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Angiogenesis assays allow for the evaluation of pro- or anti-angiogenic activity of endogenous or exogenous factors (stimulus or inhibitors) through investigation of their pro-or anti- proliferative, migratory, and tube formation effects on endothelial cells. To model the process of angiogenesis and the effects of biomolecules on that process, both in vitro and in vivo methods are currently used. In general, in vitro methods monitor specific stages in the angiogenesis process and are used for early evaluations, while in vivo methods more accurately simulate the living microenvironment to provide more pertinent information. We review here the current state of angiogenesis assays as well as their mechanisms, advantages, and limitations.

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Section: In Vitro Assaysmentioning

confidence: 99%

Section: In Vitro Assaysmentioning

confidence: 99%

Section: In Vitro Assaysmentioning

confidence: 99%

Section: In Vitro Assaysmentioning

confidence: 99%

See 2 more Smart Citations

Evaluation of Angiogenesis Assays

Stryker¹,

Rajabi

Davis

et al. 2019

Biomedicines

View full text Add to dashboard Cite

show abstract

“…Data can only be collected in cases where ECs are plated entirely without the presence of fibroblasts or cancerous cells, and the existence of lumens within the capillary-like structures should also be verified. 73 Although this is typically a two-dimensional method, it can also be performed to assess angiogenesis in three-dimensions. ECs are grown and plated between layers of Matrigel, and generally, tubes are formed horizontally between layers.…”

Section: Assessing the Angiogenic Responsementioning

confidence: 99%

Vascularization Approaches in Tissue Engineering: Recent Developments on Evaluation Tests and Modulation

Lopes

Collins

Reis

et al. 2021

ACS Appl. Bio Mater.

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This review focuses on vascularization and strategies involved in its evaluation and modulation. Clinical issues associated with engineered tissues of an atomically relevant size that require a vascular network to supply their cells with nutrients and oxygen are analyzed in terms of vascular network formation within scaffolds, which can be produced from varying biomaterials, with the capability of connecting to the vasculature of the patient. Developing angiogenesis techniques and monitoring of angiogenesis development as well as how these methods can be further utilized to tailor vascularization within large tissue engineered constructs are also discussed. Finally, we offer a glimpse toward the future by providing an outlook for vascularization and associated emerging bioprinting concepts in tissue engineering applications.

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Design, Synthesis, and Hypoxia‐Inducible Factor‐1α Inhibitory Activity Evaluation of Panaxadiol Derivatives Containing a Thiazole Moiety

Ma,

Li,

Jin

et al. 2024

Chemistry & Biodiversity

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The hypoxia‐inducible factor‐1α (HIF‐1α) pathway has been implicated in tumor angiogenesis, growth, and metastasis. Therefore, the inhibition of this pathway is an important therapeutic target for cancer. Here, three series of panaxadiol derivatives containing a thiazole moiety (5a‐l, 7a‐i, and 9a‐i) were synthesized and evaluated for HIF‐1α inhibitory activity using a Hep3B cell‐based luciferase reporter assay. Compounds 5d and 7b showed the strongest inhibitory activity with IC50 values of 17.37 and 6.42 μM, respectively, and did not show any significant cytotoxicity. Western blot assay results indicated that these two compounds exhibited more potent inhibition, compared with panaxadiol, of the expression of HIF‐1α protein in Hep3B cells at a concentration of 50 µM. Molecular docking experiments were also performed to investigate the structure–activity relationship.

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Synthesis and evaluation of N -(benzofuran-5-yl)aromaticsulfonamide derivatives as novel HIF-1 inhibitors that possess anti-angiogenic potential

Cited by 16 publications

References 36 publications

Evaluation of Angiogenesis Assays

Evaluation of Angiogenesis Assays

Vascularization Approaches in Tissue Engineering: Recent Developments on Evaluation Tests and Modulation

Design, Synthesis, and Hypoxia‐Inducible Factor‐1α Inhibitory Activity Evaluation of Panaxadiol Derivatives Containing a Thiazole Moiety

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