“…[80] Molecular docking of a few indoline-containing phenolic Mannich bases identified compound 66 (Figure 8) as the most potent inhibitor of epidermal growth factor receptor (EGFR), and its cytotoxic action on MCF-7 (IC 50 = 64.1 μM) and SkBrc (IC 50 = 120 μM) breast cancer cells was proven to be exerted via EGFR signaling pathway. [81] Along with two other aminoalkylphenols obtained through the Petasis borono-Mannich reaction, compound 67 (R = CH 3 ) (Figure 8) was also shown to inhibit the growth of LN229 and SNB19 glioblastoma cells with IC 50 values of 26.5 and 75.4 mM, respectively, and to induce G1/ S phase cell cycle arrest in glioblastoma cells through p53 and cyclin-dependent kinase signaling pathway. [82] An assessment of the potential therapeutic effects of the same compound on glioblastoma stem cells and non-stem cancer cells derived from two different glioblastoma cell lines (LN229 and SNB19), and of the underlying mechanisms in various signaling pathways has evidenced that aminoalkylphenol 67 (R = CH 3 ) (Figure 8) ar-rested the cell cycle through modulation of EGFR and cancer stem cell signaling pathways.…”
Section: Chemmedchemmentioning
confidence: 91%
“…Imaging, computational approach and biochemical methods have been employed to investigate the effect of the structural differences between compounds 66 and 67 (R=OCH 3 ) (Figure 8) on for heterogeneity, apoptosis, levels of reactive oxygen species and caspase in U2OS osteosarcoma cells treated with these aminoalkylphenols [80] . Molecular docking of a few indoline‐containing phenolic Mannich bases identified compound 66 (Figure 8) as the most potent inhibitor of epidermal growth factor receptor (EGFR), and its cytotoxic action on MCF‐7 (IC 50 =64.1 μM) and SkBrc (IC 50 =120 μM) breast cancer cells was proven to be exerted via EGFR signaling pathway [81] . Along with two other aminoalkylphenols obtained through the Petasis borono‐Mannich reaction, compound 67 (R=CH 3 ) (Figure 8) was also shown to inhibit the growth of LN229 and SNB19 glioblastoma cells with IC 50 values of 26.5 and 75.4 mM, respectively, and to induce G1/S phase cell cycle arrest in glioblastoma cells through p53 and cyclin‐dependent kinase signaling pathway [82] .…”
Section: Anticancer and Cytotoxic Activity Of Mannich Bases Derived F...mentioning
This report summarizes the latest published data on the antiproliferative action and cytotoxic activity of Mannich bases, a structurally heterogeneous category of chemical entities that includes compounds which are synthesized via the grafting of an aminomethyl function onto diverse substrates by means of the Mannich reaction. The present overview of the topic is an update to the information assembled in a previously published review that covered the literature up to 2014.
“…[80] Molecular docking of a few indoline-containing phenolic Mannich bases identified compound 66 (Figure 8) as the most potent inhibitor of epidermal growth factor receptor (EGFR), and its cytotoxic action on MCF-7 (IC 50 = 64.1 μM) and SkBrc (IC 50 = 120 μM) breast cancer cells was proven to be exerted via EGFR signaling pathway. [81] Along with two other aminoalkylphenols obtained through the Petasis borono-Mannich reaction, compound 67 (R = CH 3 ) (Figure 8) was also shown to inhibit the growth of LN229 and SNB19 glioblastoma cells with IC 50 values of 26.5 and 75.4 mM, respectively, and to induce G1/ S phase cell cycle arrest in glioblastoma cells through p53 and cyclin-dependent kinase signaling pathway. [82] An assessment of the potential therapeutic effects of the same compound on glioblastoma stem cells and non-stem cancer cells derived from two different glioblastoma cell lines (LN229 and SNB19), and of the underlying mechanisms in various signaling pathways has evidenced that aminoalkylphenol 67 (R = CH 3 ) (Figure 8) ar-rested the cell cycle through modulation of EGFR and cancer stem cell signaling pathways.…”
Section: Chemmedchemmentioning
confidence: 91%
“…Imaging, computational approach and biochemical methods have been employed to investigate the effect of the structural differences between compounds 66 and 67 (R=OCH 3 ) (Figure 8) on for heterogeneity, apoptosis, levels of reactive oxygen species and caspase in U2OS osteosarcoma cells treated with these aminoalkylphenols [80] . Molecular docking of a few indoline‐containing phenolic Mannich bases identified compound 66 (Figure 8) as the most potent inhibitor of epidermal growth factor receptor (EGFR), and its cytotoxic action on MCF‐7 (IC 50 =64.1 μM) and SkBrc (IC 50 =120 μM) breast cancer cells was proven to be exerted via EGFR signaling pathway [81] . Along with two other aminoalkylphenols obtained through the Petasis borono‐Mannich reaction, compound 67 (R=CH 3 ) (Figure 8) was also shown to inhibit the growth of LN229 and SNB19 glioblastoma cells with IC 50 values of 26.5 and 75.4 mM, respectively, and to induce G1/S phase cell cycle arrest in glioblastoma cells through p53 and cyclin‐dependent kinase signaling pathway [82] .…”
Section: Anticancer and Cytotoxic Activity Of Mannich Bases Derived F...mentioning
This report summarizes the latest published data on the antiproliferative action and cytotoxic activity of Mannich bases, a structurally heterogeneous category of chemical entities that includes compounds which are synthesized via the grafting of an aminomethyl function onto diverse substrates by means of the Mannich reaction. The present overview of the topic is an update to the information assembled in a previously published review that covered the literature up to 2014.
“…6 a 1.5% Agarose gel electrophoresis of DNA extracted from HNPMI treated and untreated cells MCF-7 cells. Lane 1—1 Kb Ladder, Lane 2—DNA of cells treated with HNPMI, Lane 3—DNA of untreated cells [ 39 ]. b SCGE showing a comet shape describes the amount of DNA in the nucleus as a head and the pattern and amount of DNA that has drifted away from the nucleus creating tail.…”
Section: Dna Fragmentation/denaturation/condensation Detection Methodsmentioning
confidence: 99%
“…The appearance of green fluorescence (white arrow) in untreated control cells represents viable cells with normal morphology whereas visualisation of bright yellow-green colour (yellow arrow) and reddish yellow/orange staining (blue arrow) in the treated cells shows the presence of early and late apoptotic cells. Necrotic cells appear as a uniform orange stain [ 39 ] …”
Section: Dna Fragmentation/denaturation/condensation Detection Methodsmentioning
Programmed cell death is considered a key player in a variety of cellular processes that helps to regulate tissue growth, embryogenesis, cell turnover, immune response, and other biological processes. Among different types of cell death, apoptosis has been studied widely, especially in the field of cancer research to understand and analyse cellular mechanisms, and signaling pathways that control cell cycle arrest. Hallmarks of different types of cell death have been identified by following the patterns and events through microscopy. Identified biomarkers have also supported drug development to induce cell death in cancerous cells. There are various serological and microscopic techniques with advantages and limitations, that are available and are being utilized to detect and study the mechanism of cell death. The complexity of the mechanism and difficulties in distinguishing among different types of programmed cell death make it challenging to carry out the interventions and delay its progression. In this review, mechanisms of different forms of programmed cell death along with their conventional and unconventional methods of detection of have been critically reviewed systematically and categorized on the basis of morphological hallmarks and biomarkers to understand the principle, mechanism, application, advantages and disadvantages of each method. Furthermore, a very comprehensive comparative analysis has been drawn to highlight the most efficient and effective methods of detection of programmed cell death, helping researchers to make a reliable and prudent selection among the available methods of cell death assay. Conclusively, how programmed cell death detection methods can be improved and can provide information about distinctive stages of cell death detection have been discussed.
An efficient and practical one‐pot reaction for the synthesis of diarylmethyl anilines from easy available materials of salicylaldehydes, arylboronic acids and aromatic amines has been successfully developed. All the reactions proceed smoothly under transition‐metal‐free conditions via a p‐TSA promoted tandem Petasis borono‐Mannich/ nucleophilic substitution reaction, providing highly functionalized amines with wide functional groups in good to excellent yields. A reasonable explanation for this transformation was suggested.
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