2--hydroxychalcone and Lung-Neoplasms

2--hydroxychalcone has been researched along with Lung-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for 2--hydroxychalcone and Lung-Neoplasms

Article	Year
Discovery of 2'-hydroxychalcones as autophagy inducer in A549 lung cancer cells. Organic & biomolecular chemistry, 2014, May-21, Volume: 12, Issue:19 A series of 2'-hydroxychalcone derivatives was synthesized and the effects of all the compounds on growth of A549 lung cancer cell were investigated. The results showed that all compounds had inhibitory effects on the growth of A549 lung cancer cells and compound possessed the highest growth inhibitory effect and induced autophagy of A549 lung cancer cells. Topics: Apoptosis; Autophagy; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Cell Shape; Chalcones; Drug Discovery; Humans; Inhibitory Concentration 50; L-Lactate Dehydrogenase; Lung Neoplasms; Microtubule-Associated Proteins; Necrosis	2014
Structure-activity relationship studies of chalcone leading to 3-hydroxy-4,3',4',5'-tetramethoxychalcone and its analogues as potent nuclear factor kappaB inhibitors and their anticancer activities. Journal of medicinal chemistry, 2009, Nov-26, Volume: 52, Issue:22 Chalcone is a privileged structure, demonstrating promising anti-inflammatory and anticancer activities. One potential mechanism is to suppress nuclear factor kappa B (NF-kappaB) activation. The structures of chalcone-based NF-kappaB inhibitors vary significantly that there is minimum information about their structure-activity relationships (SAR). This study aims to establish SAR of chalcone-based compounds to NF-kappaB inhibition, to explore the feasibility of developing simple chalcone-based potent NF-kappaB inhibitors, and to evaluate their anticancer activities. Three series of chalcones were synthesized in one to three steps with the key step being aldol condensation. These candidates demonstrated a wide range of NF-kappaB inhibitory activities, some of low micromolar potency, establishing that structural complexity is not required for NF-kappaB inhibition. Lead compounds also demonstrate potent cytotoxicity against lung cancer cells. Their cytotoxicities correlate moderately well with their NF-kappaB inhibitory activities, suggesting that suppressing NF-kappaB activation is likely responsible for at least some of the cytotoxicities. One lead compound effectively inhibits lung tumor growth with no signs of adverse side effects. Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Cell Transformation, Neoplastic; Chalcone; Chalcones; Female; Genes, Reporter; Humans; I-kappa B Kinase; Inhibitory Concentration 50; Interleukin-1 Receptor-Associated Kinases; Luciferases; Lung Neoplasms; Mice; Mice, Nude; NF-kappa B; Structure-Activity Relationship; Tumor Necrosis Factor-alpha	2009

Article

Year

Discovery of 2'-hydroxychalcones as autophagy inducer in A549 lung cancer cells.

Organic & biomolecular chemistry, 2014, May-21, Volume: 12, Issue:19

A series of 2'-hydroxychalcone derivatives was synthesized and the effects of all the compounds on growth of A549 lung cancer cell were investigated. The results showed that all compounds had inhibitory effects on the growth of A549 lung cancer cells and compound possessed the highest growth inhibitory effect and induced autophagy of A549 lung cancer cells.

Topics: Apoptosis; Autophagy; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Cell Shape; Chalcones; Drug Discovery; Humans; Inhibitory Concentration 50; L-Lactate Dehydrogenase; Lung Neoplasms; Microtubule-Associated Proteins; Necrosis

2014

Structure-activity relationship studies of chalcone leading to 3-hydroxy-4,3',4',5'-tetramethoxychalcone and its analogues as potent nuclear factor kappaB inhibitors and their anticancer activities.

Journal of medicinal chemistry, 2009, Nov-26, Volume: 52, Issue:22

Chalcone is a privileged structure, demonstrating promising anti-inflammatory and anticancer activities. One potential mechanism is to suppress nuclear factor kappa B (NF-kappaB) activation. The structures of chalcone-based NF-kappaB inhibitors vary significantly that there is minimum information about their structure-activity relationships (SAR). This study aims to establish SAR of chalcone-based compounds to NF-kappaB inhibition, to explore the feasibility of developing simple chalcone-based potent NF-kappaB inhibitors, and to evaluate their anticancer activities. Three series of chalcones were synthesized in one to three steps with the key step being aldol condensation. These candidates demonstrated a wide range of NF-kappaB inhibitory activities, some of low micromolar potency, establishing that structural complexity is not required for NF-kappaB inhibition. Lead compounds also demonstrate potent cytotoxicity against lung cancer cells. Their cytotoxicities correlate moderately well with their NF-kappaB inhibitory activities, suggesting that suppressing NF-kappaB activation is likely responsible for at least some of the cytotoxicities. One lead compound effectively inhibits lung tumor growth with no signs of adverse side effects.

Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Cell Transformation, Neoplastic; Chalcone; Chalcones; Female; Genes, Reporter; Humans; I-kappa B Kinase; Inhibitory Concentration 50; Interleukin-1 Receptor-Associated Kinases; Luciferases; Lung Neoplasms; Mice; Mice, Nude; NF-kappa B; Structure-Activity Relationship; Tumor Necrosis Factor-alpha

2009