Synthesis and Anxiolytic Activity of Some Novel 5-oxo-1, 4-oxazepine Derivatives

AbdelFattah, Bothiana A.; Khalifa, Maha M.; El‐Sehrawi, Hend M.; Fayed, Eman A.; Bayoumi, Ashraf H.; Said, M. M.

doi:10.2174/157018011794839448

Cited by 16 publications

(6 citation statements)

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“…Based on the above findings, and in continuation to our work on the synthesis of new compounds with biological activities [28][29][30][31][32][33][34], we have synthesized a new series of quinolone-3-carboxamide derivatives containing a series of biologically active moites that are expected to be strongly inhibitory for several human cell lines and PIM-1 inhibitors as a result of our commitment to search for new potential anticancer agents related to heterocyclic [35][36][37][38][39][40][41][42]. | P a g e…”

Section: Figure 1: Structures For Pim-1 Inhibitors and The Newly Designed Quinoline Hybridsmentioning

confidence: 99%

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

et al. 2021

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The targeted approach of protein kinases (PKs), as PKs are the main regulators of cell survival and proliferation, has been a promising strategy for treatments for cancer. Here we analyze the potential of quinoline-carboximide derivatives for four cell lines: MCF-7, CACO, HepG-2 and HCT-116 as anticancer agents. 3e, 4b, 11b and 13d derivatives showed good anti-proliferative activities in comparison to the reference standard Doxorubicin, against the four cell lines tested. They have been chosen for further studies. First of all, the IC50 value surveys were carried out to ensure the protection of our hits and demonstrate that the cytotoxic effect (IC50 > 113 μM) is highly selective on normal human cells (WI-38). Secondly, apoptosis was accomplished by down-regulation of Bcl-2 and up-regulation of BAX and Caspase-3 by these active compounds. Also, the Pim-1 inhibitory activity of the active hybrids was done, which indicate that compound 3e was the most active with percentage of inhibition 82.27% and IC50 equal 0.11 when compaired to SGI-1776 as a reference standered. In addition, the in silico assessment of ADME properties, all of the strongest compounds are orally bioavailable without blood brain barrier penetration.

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Section: Figure 1: Structures For Pim-1 Inhibitors and The Newly Designed Quinoline Hybridsmentioning

confidence: 99%

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

et al. 2021

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“…Depending on the previous results and in continuation of our previous efforts in designing new heterocyclic compounds having biological activity [53][54][55][56][57][58][59]. Based on the aforementioned data regarding the biological significance of both pyrazolo-pyrimidines, Fluorine, and azo group moieties, it was conceptualized that the tethering of these pharmacophores in one scaffold using a fragment-based drug design approach would be of great interest to develop highly potent anticancer agents.…”

Section: Introductionmentioning

confidence: 99%

Novel fluorinated pyrazole-based heterocycles scaffold: cytotoxicity, in silico studies and molecular modelling targeting double mutant EGFR L858R/T790M as antiproliferative and apoptotic agents

Fayed

Gohar²,

Bayoumi

et al. 2023

Med Chem Res

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Hepatocellular carcinoma (HCC), also known as hepatoma, is the most prevalent type of primary liver cancer. It begins in the hepatocytes, the liver’s major cell type. Cancer that began in another region of the body but has spread to the liver is known as secondary cancer of life; several still unmet demands for better, less toxic therapy to treat this malignant tumor. Several novel pyrazolo[1,5-a]pyrimidine derivatives were synthesized as part of our goal to develop promising anticancer drugs. All the synthesized hybrids have been screened for their cytotoxicity effect against three cancer cell lines which are; HepG-2, HCT-116, and MCF-7. The liver cancer cells were found to be the most sensitive to the effect of the new molecules. A subsequent set of in vitro biological evaluation studies has been conducted on the most promising derivatives to identify their effect on such a cancer type. In HepG-2 cells, four derivatives (8a, 8b, 10c, and 11b) demonstrated good anticancer activity. The most efficacious compounds were 8b and 10c, which had IC50 values of 2.36 ± 0.14 and 1.14 ± 0.063 μM, respectively, higher than the reference medication Imatinib. The latter’s putative molecular effect has been investigated further by looking at its influence on the cell cycle, EGFR, and specific apoptotic and anti-apoptotic markers in HepG-2 cells. These findings indicated that 8b and 10c could trigger apoptosis by upregulating BAX and caspase-3 and cell cycle at the Pre-G1 and G2-M stages. The compounds 8b and 10c showed high potency for EGFR with IC50 equal to 0.098 and 0.079 μM, respectively. Compound 10c had the most effective inhibitory activity for EGFR L858R-TK with IC50 (36.79 nM). Additionally, in silico ADMET and docking studies were done for the most active hits, representing good results. Graphical Abstract

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“…Schiff bases are compounds prepared from the reaction of aldehydes or ketones with amines. The azomethine group has replaced the carbonyl group, and the nitrogen atom is attached to an aryl or alkyl (1). They are antimicrobial (2), antituberculosis (3), anti-cancer (4), antioxidant (5), anti-inflammatory (6), antifungal (7), and corrosion inhibitors (8).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and cytotoxicity evaluation of pyrazole compounds bearing oxazepine core against breast cancer cells

Azzawi

Hussein

2022

ijhs

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The research included the preparation of two Schiff bases MA1,2 starting from1-methyl-pyrazole-4-carbaldehyde with 4-chloroaniline or 4-amino antipyrine in equal moles in the presence of glacial acetic acid. Then xazepane rings MA (3-6) were prepared from MA1,2 with phthalic anhydride or maleic anhydride. The prepared chemical formulas were confirmed using FTIR, 1HNMR, and 13CNMR spectroscopy. The toxicity activity of the compound MA2 against breast cancer MDA and REF cells was tested at seven concentrations (400, 200, 100, 50, 25, 12.5, 6.25) ml/ µg. The study also showed the lowest inhibition rate for MDA cancer line cells at 6.25 µg/ml by (4%) and the highest inhibition rate at 400 µg/ml by 77%, and the study showed the compound with the highest toxicity in healthy cells (64%-80%).

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Synthesis and Anxiolytic Activity of Some Novel 5-oxo-1, 4-oxazepine Derivatives

Cited by 16 publications

References 0 publications

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

Carboxamide appended quinoline moieties as potential anti-proliferative agents, apoptotic inducers and Pim-1 kinase inhibitors

Novel fluorinated pyrazole-based heterocycles scaffold: cytotoxicity, in silico studies and molecular modelling targeting double mutant EGFR L858R/T790M as antiproliferative and apoptotic agents

Synthesis and cytotoxicity evaluation of pyrazole compounds bearing oxazepine core against breast cancer cells

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