127034-12-2Relevant academic research and scientific papers
CHALCONE DERIVATIVES AS NRF2 ACTIVATORS
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Page/Page column 56, (2012/09/11)
Compounds and methods for treating or preventing a disease, disorder or condition associated with an Nrf2-regulated pathway, including those associated with an autoimmune disease, comorbidity associated with diabetes, such as retinopathy and nephropathy, bone marrow transplant for leukemia and related cancers, bone marrow deficiencies, inborn errors of metabolism, and other immune disorders, oxidative stress, respiratory infection, ischemia, neurodegenerative disorders, radiation injury, neutropenia caused by chemotherapy, autoimmunity, and congenital neutropenic disorders, and for restoring a corticosteroid responsiveness, in a subject are provided.
Novel chalcone derivatives as potent Nrf2 activators in mice and human lung epithelial cells
Kumar, Vineet,Kumar, Sarvesh,Hassan, Mohammad,Wu, Hailong,Thimmulappa, Rajesh K.,Kumar, Amit,Sharma, Sunil K.,Parmar, Virinder S.,Biswal, Shyam,Malhotra, Sanjay V.
experimental part, p. 4147 - 4159 (2011/08/03)
Nrf2-mediated activation of antioxidant response element is a central part of molecular mechanisms governing the protective function of phase II detoxification and antioxidant enzymes against carcinogenesis, oxidative stress, and inflammation. Nrf2 is sequestered in the cytoplasm by its repressor, Keap1. We have designed and synthesized novel chalcone derivatives as Nrf2 activators. The potency of these compounds was measured by the expression of Nrf2 dependent antioxidant genes GCLM, NQO1, and HO1 in human lung epithelial cells, while the cytotoxicity was analyzed using MTT assay. In vivo potency of identified lead compounds to activate Nrf2 was evaluated using a mouse model. Our studies showed 2-trifluoromethyl-2′-methoxychalone (2b) to be a potent activator of Nrf2, both in vitro and in mice. Additional experiments showed that the activation of Nrf2 by this compound is independent of reactive oxygen species or redox changes. We have discussed a quantitative structure-activity relationship and proposed a possible mechanism of Nrf2 activation.
Chalcones: A new class of antimitotic agents
Edwards,Stemerick,Sunkara
, p. 1948 - 1954 (2007/10/02)
A series of chalcones was evaluated as antimitotic agents. One of these, (E)-1-(2,5-dimethoxyphenyl)-3-[4-(dimethylamino)phenyl]-2-methyl-2-propen- 1-one) (73), was found to be an effective antimitotic agent at a concentration of 4 nM in an in vitro HeLa
