Synthesis of some novel 4-benzothiazol-2-yl-benzoyl-1H-pyrazoles, and evaluation as antiangiogenic agents

El‐Meguid, Eman A. Abd; Ali, Mamdouh M.

doi:10.1007/s11164-015-2100-8

Cited by 17 publications

(7 citation statements)

References 36 publications

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“…Pyrazoles were clubbed with different other functional groups or heterocycles to generate hybrid molecules and they are found to exhibit various biological activities, such as anti-inflammatory, [23] antibacterial, [24] antitubercular, [25] analgesic, [26] anticancer, [27] and antiangiogenic. [28] However, pyrazole-based compounds are less explored for their antidiabetic potency except for a few marked reports. Notably, compound 5 emerged as PPAR-γ and antiamylase agent [29] and 6 as a potent α-amylase inhibitor (Figure 1).…”

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confidence: 99%

In vitro and in silico studies of fluorinated 2,3‐disubstituted thiazolidinone‐pyrazoles as potential α‐amylase inhibitors and antioxidant agents

Ganavi

Ramu

Kumar

et al. 2021

Archiv der Pharmazie

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As part of our effort to identify potent α-amylase inhibitors, in the present study, a novel series of fluorinated thiazolidinone-pyrazole hybrid molecules were prepared by the condensation of 3-(aryl/benzyloxyaryl)-pyrazole-4-carbaldehydes with fluorinated 2,3disubstituted thiazolidin-4-ones. The structures of the newly synthesized compounds were confirmed by infrared, 1 H nuclear magnetic resonance (NMR), 13 C NMR, and liquid chromatography-mass spectrometry data. All the compounds were screened for their αamylase inhibitory and free radical scavenging activities by DPPH (1,1-diphenyl-2picrylhydrazyl) and ABTS methods. Among the tested compounds, compound 8g emerged as a promising α-amylase inhibitor with IC 50 = 0.76 ± 1.23 µM, and it was found to be more potent than the standard drug acarbose (IC 50 = 0.86 ± 0.81 μM). Compounds 8b and 8g showed strong free radical scavenging activity compared to the standard butylated hydroxyl anisole. The kinetic study of compound 8g revealed the reversible, classical competitive inhibition mode on the α-amylase enzyme. Molecular docking and dynamic simulations studies were performed for the most potent compound 8g, which displayed remarkable hydrogen bonding with the α-amylase protein (PDB ID: 1DHK).

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confidence: 99%

In vitro and in silico studies of fluorinated 2,3‐disubstituted thiazolidinone‐pyrazoles as potential α‐amylase inhibitors and antioxidant agents

Ganavi

Ramu

Kumar

et al. 2021

Archiv der Pharmazie

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“…To study the in vivo safety and biocompatibility, blood of all mice was collected on the 14th day of treatment (Tables S10 and S11). Blood routine and biochemistry indicators, blood urea nitrogen (BUN), including aspartate aminotransferase (AST), creatinine (CREA), alkaline phosphatase (ALP), alanine aminotransferase (ALT), and white blood cell (WBC) count, etc., 50 are shown in Figure 8. As one of the main side effects of cisplatin, the mice hatched with cisplatin show a significant decrease in the WBC count and absolute value of monocytes in this study (Figure 8a), which suggests the occurrence of myelosuppression.…”

Section: Resultsmentioning

confidence: 99%

In Vitro and In Vivo of Triphenylamine-Appended Fluorescent Half-Sandwich Iridium(III) Thiosemicarbazones Antitumor Complexes

et al. 2021

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Half-sandwiched structure iridium(III) complexes appear to be an attractive organometallic antitumor agents in recent years. Here, four triphenylamine-modified fluorescent half-sandwich iridium(III) thiosemicarbazone (TSC) antitumor complexes were developed. Because of the “enol” configuration of the TSC ligands, these complexes formed a unique dimeric configuration. Aided by the appropriate fluorescence properties, studies found that complexes could enter tumor cells in an energy-dependent mode, accumulate in lysosomes, and result in the damage of lysosome integrity. Complexes could block the cell cycle, improve the levels of intrastitial reactive oxygen species, and lead to apoptosis, which followed an antitumor mechanism of oxidation. Compared with cisplatin, the antitumor potential in vivo and vitro confirmed that Ir4 could effectively inhibit tumor growth. Meanwhile, Ir4 could avoid detectable side effects in the experiments of safety evaluation. Above all, half-sandwich iridium(III) TSC complexes are expected to be an encouraging candidate for the treatment of malignant tumors.

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“…Some compounds (comprising 5-pyrazolyl derivatives 33, Figure 5) showed promising cytotoxic activity against breast cancer cell line MCF-7 and inhibited human VEGF in MCF-7 cancer cell lines with comparable activity of reference compound tamoxifen [77].…”

Section: -Pyrazolyl-ureas As Antiangiogenic Agentsmentioning

confidence: 99%

Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry

2020

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The pyrazole nucleus has long been known as a privileged scaffold in the synthesis of biologically active compounds. Within the numerous pyrazole derivatives developed as potential drugs, this review is focused on molecules characterized by a urea function directly linked to the pyrazole nucleus in a different position. In the last 20 years, the interest of numerous researchers has been especially attracted by pyrazolyl-ureas showing a wide spectrum of biological activities, ranging from the antipathogenic activities (bacteria, plasmodium, toxoplasma, and others) to the anticarcinogenic activities. In particular, in the anticancer field, pyrazolyl-ureas have been shown to interact at the intracellular level on many pathways, in particular on different kinases such as Src, p38-MAPK, TrKa, and others. In addition, some of them evidenced an antiangiogenic potential that deserves to be explored. This review therefore summarizes all these biological data (from 2000 to date), including patented compounds.

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Synthesis of some novel 4-benzothiazol-2-yl-benzoyl-1H-pyrazoles, and evaluation as antiangiogenic agents

Cited by 17 publications

References 36 publications

In vitro and in silico studies of fluorinated 2,3‐disubstituted thiazolidinone‐pyrazoles as potential α‐amylase inhibitors and antioxidant agents

In vitro and in silico studies of fluorinated 2,3‐disubstituted thiazolidinone‐pyrazoles as potential α‐amylase inhibitors and antioxidant agents

In Vitro and In Vivo of Triphenylamine-Appended Fluorescent Half-Sandwich Iridium(III) Thiosemicarbazones Antitumor Complexes

Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry

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