2017
DOI: 10.1016/j.ejmech.2017.07.056
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Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells

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Cited by 21 publications
(9 citation statements)
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“…The different substituted pyrazole carbaldehydes ( 12a–d ) and substituted pyrazole hydrazides ( 10a–e ) used in this study were adopted from our previous reports (Kamal et al., ; Shaik et al., ). To the substituted pyrazole‐5‐carbaldehyde ( 12a ) prepared in the previous step was added to the corresponding substituted pyrazole hydrazide in ethanol in presence of catalytic amount of glacial acetic acid.…”
Section: Methodsmentioning
confidence: 99%
“…The different substituted pyrazole carbaldehydes ( 12a–d ) and substituted pyrazole hydrazides ( 10a–e ) used in this study were adopted from our previous reports (Kamal et al., ; Shaik et al., ). To the substituted pyrazole‐5‐carbaldehyde ( 12a ) prepared in the previous step was added to the corresponding substituted pyrazole hydrazide in ethanol in presence of catalytic amount of glacial acetic acid.…”
Section: Methodsmentioning
confidence: 99%
“…Pyrazole can be synthesized in a variety of ways, such as by Knorr reaction or through the pyrazoline pathway, which is the reaction of α, β-unsaturated ketone with hydrazine derivatives [8] or semicarbazide [9], followed by oxidative aromatization to the corresponding pyrazole molecules [10]. Some studies have also reported that pyrazole derivatives also exhibit anti-cancer activity against breast cancer cell lines [11,12]. Furthermore, many pyrazoles have been patented as hepatic cancer (HePG-2) agents [13], and celecoxib is a commercial drug with cyclooxygenase-2 inhibitory activity [14].…”
Section: Introductionmentioning
confidence: 99%
“…28,29 Recent studies have reported that the expression level of PTEN was related to miR-21, which facilitated the activation of the phosphatidylinositol 3-kinase (PI3K)/Akt pathway by restraining PTEN, 30−32 while the high activity of Akt and its downstream factors induced insensitivity of drugresistant cells to chemotherapy drugs. 33,34 As aforementioned, the sensitivity of cells to chemotherapeutic drugs may be increased by the miRNA-21 inhibitor (anti-miR-21).…”
Section: ■ Introductionmentioning
confidence: 99%
“…So far, a lot of work has demonstrated that microRNAs (miRNAs) acted as regulators of P-gp gene expression in various cancer types and played an important role in reversing MDR. MiRNAs served as a kind of endogenous single-stranded RNA molecules, which are corrected with the progresses of cytodifferentiation, proliferation, apoptosis, and antiviral defense of cancer. , Recently, it has been reported that regulation of miRNA expression exerted essential roles in inhibiting tumor progression and invasion. , MiRNAs could also have a significant effect on the sensitivity of tumor cells to chemotherapeutic drugs . Among them, microRNA-21 (miR-21), an important crucial oncogenic miRNA, has the advantage of promoting cell invasion by regulating various genes, including the programmed cell death 4 (PDCD4) gene, tissue inhibitor of metallopeptidase inhibitor 3 (TIMP3), phosphatase, and tensin homologue (PTEN) gene in a variety of tumors, such as lung cancer, glioblastoma, and breast cancer. , Recent studies have reported that the expression level of PTEN was related to miR-21, which facilitated the activation of the phosphatidylinositol 3-kinase (PI3K)/Akt pathway by restraining PTEN, while the high activity of Akt and its downstream factors induced insensitivity of drug-resistant cells to chemotherapy drugs. , As aforementioned, the sensitivity of cells to chemotherapeutic drugs may be increased by the miRNA-21 inhibitor (anti-miR-21).…”
Section: Introductionmentioning
confidence: 99%