scholarly journals Design, synthesis and anticancer activity of furochromone and benzofuran derivatives targeting VEGFR-2 tyrosine kinase

RSC Advances ◽  
2015 ◽  
Vol 5 (32) ◽  
pp. 25312-25324 ◽  
Author(s):  
Omaima M. Abdelhafez ◽  
Hamed I. Ali ◽  
Kamelia M. Amin ◽  
Mohamed M. Abdalla ◽  
Eman Y. Ahmed
Keyword(s):  
Tyrosine Kinase ◽  
Anticancer Activity ◽  
Design Synthesis ◽  
Cancer Activity

Furochromone and benzofuran derivatives were synthesized, docked and evaluated for their anti-VEGFR-2 activity, cytotoxicity, and in vivo antiprostate cancer activity.

scholarly journals Recent study on the anticancer activity of nobiletin and its metabolites

2021 ◽  
Vol 14 ◽  
Author(s):  
Ke Lv ◽  
Lingling Zhang ◽  
Hui Zhao ◽  
Chi-Tang Ho ◽  
Shiming Li
Keyword(s):  
Cancer Prevention ◽  
Anticancer Activity ◽  
Promising Candidate ◽  
Naturally Occurring ◽  
Antitumor Potential ◽  
Anti Cancer ◽  
Citrus Peels ◽  
Derivatives Of ◽  
Cancer Activity

The exploration of naturally occurring phytochemicals with antitumor potential has been the focus of many studies. Nobiletin, a polymethoxyflavone (PMF) exclusively derived from citrus peels, has been reported as a promising candidate for the prevention and/or treatment of cancers. Additionally, multiple demethylated derivatives of nobiletin from in vivo biotransformation, including 3′-demethylnobiletin (3′-DMN), 4′-demethylnobiletin (4′-DMN), 3′,4′-didemethylnobiletin (3′,4′-DDMN) and 5-demethylnobiletin (5-DMN), among others, have been found to show anti-cancer activity. In this review, the anticancer activity of nobiletin and its derivatives in cancer prevention are comprehensively described.

Design, Synthesis and Anti-breast Cancer Activity of Some Novel Substituted Isoxazoles as Anti-breast Cancer Agent

2018 ◽  
Vol 18 (7) ◽  
pp. 1009-1015
Author(s):  
Santosh N. Mokale ◽  
Nikhil S. Sakle ◽  
Swati A. Bhavale ◽  
Deepak K. Lokwani ◽  
Vishakha R. Shelke
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Virgin Female ◽  
Cancer Cell Line ◽  
Breast Cancer Cell Lines ◽  
Sprague Dawley ◽  
Design Synthesis

Methods: A novel series of isoxazole (S21-S30) derivatives were designed, synthesized and screened for their anticancer activity against estrogen receptor-positive MCF-7 and negative MDA-MB-435 breast cancer cell lines. The synthesized derivative has the ability to inhibit the growth of the human breast cancer cell line at low concentrations. In vivo anticancer activity was performed on virgin female sprague dawley rats. Results: The result shows that compound S23 has more selectivity and marked estrogen modulator activity than the standard tamoxifen.

Design, synthesis and in vivo anticancer activity of novel parthenolide and micheliolide derivatives as NF-κB and STAT3 inhibitors

2021 ◽  
Vol 111 ◽  
pp. 104973
Author(s):  
Binglin Zeng ◽  
Yu Cheng ◽  
Kailu Zheng ◽  
Shuoxiao Liu ◽  
Longying Shen ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Design Synthesis

Design, synthesis and anticancer activity of benzofuran derivatives targeting VEGFR-2 tyrosine kinase

RSC Advances ◽  
2014 ◽  
Vol 4 (23) ◽  
pp. 11569 ◽  
Author(s):  
Omaima M. Abdelhafez ◽  
Kamelia M. Amin ◽  
Hamed I. Ali ◽  
Mohamed M. Abdalla ◽  
Eman Y. Ahmed
Keyword(s):  
Tyrosine Kinase ◽  
Anticancer Activity ◽  
Design Synthesis

scholarly journals Melatonin Synergizes with Sorafenib to Suppress Pancreatic Cancer via Melatonin Receptor and PDGFR-β/STAT3 Pathway

2018 ◽  
Vol 47 (5) ◽  
pp. 1751-1768 ◽  
Author(s):  
Zhenghuan Fang ◽  
Kyung Hee Jung ◽  
Hong Hua Yan ◽  
Soo-Jung Kim ◽  
Marufa Rumman ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Anticancer Activity ◽  
Signaling Pathway ◽  
Xenograft Model ◽  
Proximity Ligation Assay ◽  
Melatonin Receptor ◽  
Stat3 Signaling ◽  
Stat3 Signaling Pathway

Background/Aims: Pancreatic ductal adenocarcinoma (PDAC) is one of the most lethal malignant tumors with poor prognosis. Conventional chemotherapies including gemcitabine have failed owing to weak response and side effects. Hence novel treatment regimens are urgently needed to improve the therapeutic efficacy. In this study, we aimed to assess the anticancer activity of melatonin and sorafenib as a novel therapy against PDAC. Methods: We used various apoptosis assay and PDAC xenograft model to assess anticancer effect in vitro and in vivo. We applied phospho-receptor tyrosine kinase (RTK) array and phospho-tyrosine kinase array to explore the mechanism of the combined therapy. Western blotting, proximity ligation assay, and immunoprecipitation assay were also performed for validation. Results: Melatonin synergized with sorafenib to suppress the growth of PDAC both in vitro and in vivo. The effect was due to increased apoptosis rate of PDAC cells that was accompanied by mitochondria dysfunction. The enhanced anticancer efficacy by the co-treatment could be explained by blockade of PDGFR-β/STAT3 signaling pathway and melatonin receptor (MT)-mediated STAT3. Conclusions: Melatonin reinforces the anticancer activity of sorafenib by downregulation of PDGFR-β/STAT3 signaling pathway and melatonin receptor (MT)-mediated STAT3. The combination of the two agents might be a potential therapeutic strategy for treating PDAC.

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