363618-86-4Relevant academic research and scientific papers
The synthesis of chalcones as anticancer prodrugs and their bioactivation in CYP1 expressing breast cancer cells
Ruparelia, Ketan C.,Zeka, Keti,Ijaz, Taeeba,Ankrett, Dyan N.,Wilsher, Nicola E.,Butler, Paul C.,Tan, Hoon L.,Lodhi, Sabahat,Bhambra, Avninder S.,Potter, Gerard A.,Arroo, Randolph R.J.,Beresford, Kenneth J.M.
, p. 322 - 332 (2018/06/26)
Background: Although the expression levels of many P450s differ between tumour and corresponding normal tissue, CYP1B1 is one of the few CYP subfamilies which is significantly and consistently overexpressed in tumours. CYP1B1 has been shown to be active within tumours and is capable of metabolising a structurally diverse range of anticancer drugs. Because of this, and its role in the activation of procarcinogens, CYP1B1 is seen as an important target for anticancer drug development. Objective: To synthesise a series of chalcone derivatives based on the chemopreventative agent DMU-135 and investigate their antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1. Method: A series of chalcones were synthesised in yields of 43-94% using the Claisen-Schmidt condensation reaction. These were screened using a MTT assay against a panel of breast cancer cell lines which have been characterised for CYP1 expression. Result: A number of derivatives showed promising antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1, while showing significantly lower toxicity towards a non-tumour breast cell line with no CYP expression. Experiments using the CYP1 inhibitors acacetin and α-naphthoflavone provided supporting evidence for the involvement of CYP1 enzymes in the bioactivation of these compounds. Conclusion: Chalcones show promise as anticancer agents with evidence suggesting that CYP1 activation of these compounds may be involved.
Stereoselective palladium-catalyzed α-arylation of 3-aryl-1-indanones: An asymmetric synthesis of (+)-pauciflorol F
Lee, Bong Hyang,Choi, Young Lok,Shin, Seunghoon,Heo, Jung-Nyoung
experimental part, p. 6611 - 6618 (2011/10/02)
Highly stereoselective, palladium-catalyzed α-arylation reactions of 3-aryl-1-indanones with aryl bromides are described. The use of sodium tert-butoxide as a base in this process is required to elevate the efficiencies and stereoselectivities of these re
Substituted chalcones as therapeutic compounds
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, (2008/06/13)
This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and wh
