30925-62-3

Upstream product

• 123-11-5 4-methoxy-benzaldehyde 
• 829-20-9 2',4'-dimethoxyacetophenone 
• 961-29-5 isoliquirtigenin 
• 74-88-4 methyl iodide 
• 13351-10-5 2',4'-dihydroxy-4-methoxychalcone 
• 51828-10-5 2'-methoxyisoliquiritigenin 
• 696-62-8 para-iodoanisole 
• 67756-04-1 1-(2,4-dimethoxy-phenyl)-prop-2-en-1-one 
• 151-10-0 1,3-Dimethoxybenzene 
• 637-69-4 4-Methoxystyrene 
• 20469-63-0 1-iodo-2,4-dimethoxybenzene 
• 82102-37-2 9-methyl-9H-fluorene-9-carbonyl chloride 
• 943-89-5 (E)-3-(4-methoxyphenyl)acrylic acid 
• 3179-10-0 (E)-1-methoxy-4-(2-nitrovinyl)benzene 

Downstream Products

• 40321-75-3 αβ-epoxy-2',4,4'-trimethoxydihydrochalcone 
• 93903-83-4 1-(2,4-dimethoxyphenyl)-3-(4-methoxyphenyl)propan-1-one 
• 30251-89-9 2',4,4'-Trimethoxy-3-nitro-chalcon 
• 30071-40-0 2',4,4'-Trimethoxy-3,5'-dinitro-chalcon 
• 740861-93-2 5-(2,4-dimethoxy-phenyl)-3-(4-methoxy-phenyl)-5-oxo-2-(4-oxo-4,5-dihydro-thiazol-2-yl)-pentanenitrile 
• 223389-76-2 4-(4-methoxyphenyl)-3,5-dimethyl-1,7-diphenyl-4,7-dihydro-1H-pyrano[2,3-c:6,5-c']dipyrazole 
• 740861-78-3 4-[3-(2,4-dimethoxy-phenyl)-1-(4-methoxy-phenyl)-3-oxo-propyl]-2,5-diphenyl-2,4-dihydro-pyrazol-3-one 
• 740861-74-9 4-(4-methoxy-phenyl)-1,3,5,7-tetraphenyl-4,7-dihydro-1H-pyrano[2,3-c;6,5-c']dipyrazole 
• 51813-59-3 2,5,2',5'-tetraphenyl-1,2,1',2'-tetrahydro-4,4'-(4-methoxy-phenylmethanediyl)-bis-pyrazol-3-one 
• 75436-96-3 5-(2,4-dimethoxy-phenyl)-3-(4-methoxy-phenyl)-5-oxo-valeric acid 
• 88689-02-5 5,5'-dimethyl-2,2'-diphenyl-1,2,1',2'-tetrahydro-4,4'-(4-methoxy-phenylmethanediyl)-bis-pyrazol-3-one 
• 740861-94-3 2-amino-6-(2,4-dimethoxyphenyl)-4-(4-methoxyphenyl)-3-(4-oxothiazolidin-2-yl)pyridine 

Relevant academic research and scientific papers

Application of human PCID2 protein in preparation or screening of anti-tumor drugs and compound with anti-tumor activity

The invention belongs to the technical field of biotechnology and gene therapy, and particularly relates to application of human PCID2 protein in preparation or screening of anti-tumor drugs and an anti-tumor compound. It is found that the PCID2 gene promotes tumor cell proliferation and regulates the cell cycle, is a key molecule for regulating tumor generation and development, and can be used as a target protein for preparing or screening anti-tumor drugs; meanwhile, human PCID2 protein is used as target protein, a class of PCID2 protein targeting antitumor compounds are screened out through a molecular docking technology, and the compounds can significantly inhibit tumor cell proliferation and promote tumor cell apoptosis.

The synthesis of chalcones as anticancer prodrugs and their bioactivation in CYP1 expressing breast cancer cells

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.

Visible Light Activated Radical Denitrative Benzoylation of β-Nitrostyrenes: A Photocatalytic Approach to Chalcones

A metal-free, convenient photocatalytic approach to chalcones from β-nitrostyrenes and benzaldehydes via a radical denitrative benzoylation pathway is reported. The salient features of the protocol include the utilization of visible light as an inexpensive and ecosustainable energy source, N-hydroxyphthalimide (NHPI) as a reusable organophotocatalyst and acetonitrile as an acceptable green solvent to afford chalcones in excellent yields at room temperature in a one-pot procedure. Notably, this is the first application of β-nitrostyrenes as readily available substrates for chalcone synthesis and the first example of photocatalysis in this field. (Figure presented.).

METHOD FOR PRODUCING LIQUIRITIGENIN PRECURSOR

An objective of this invention is to provide a mass manufacturing method for providing liquiritigenin by a proper method. The present invention provides a method for producing isoliquiritigenin by bringing a 4-alkoxy cinnamic acid represented by formula (I) and a 1,3-alkoxybenzene represented by formula (II) into Friedel-Crafts reaction (A) for coupling to a trialkoxy isoliquiritigenin represented by a synthesis formula (III) and allowing it to be crystal, and removing protection group to obtain an isoliquiritigenin represented by formula (IV), wherein, an in situ liquiritigenin (-) pharmacological effect is obtained by administrating the isoliquiritigenin represented by formula (IV)as a precursor of liquiritigenin into body.

Total synthesis and assignment of the absolute stereochemistry of xanthoangelol J: Development of a highly efficient method for Claisen-Schmidt condensation Dedicated to Late (Dr.) Jadab C. Sarma on his 55th birthday on first May 2013

The first total synthesis of cancer chemopreventive terpenyl hydroxychalcone xanthoangelol J isolated from Angelica keiskei was accomplished with asymmetric epoxidation, aromatic C-alkylation and Claisen-Schmidt condensation via enol mode as key steps. The crucial Claisen-Schmidt condensation has been accomplished by a novel green method using KHSO 4-SiO2 as a recyclable catalyst under microwave activation. The absolute configuration of the molecule was also determined.

Investigation of chalcones and benzochalcones as inhibitors of breast cancer resistance protein

Breast cancer resistance protein (BCRP/ABCG2) belongs to the ATP binding cassette family of transport proteins. BCRP has been found to confer multidrug resistance in cancer cells. A strategy to overcome resistance due to BCRP overexpression is the investigation of potent and specific BCRP inhibitors. The aim of the current study was to investigate different multi-substituted chalcones for their BCRP inhibition. We synthesized chalcones and benzochalcones with different substituents (viz. OH, OCH3, Cl) on ring A and B of the chalcone structure. All synthesized compounds were tested by Hoechst 33342 accumulation assay to determine inhibitory activity in MCF-7 MX and MDCK cells expressing BCRP. The compounds were also screened for their P-glycoprotein (P-gp) and Multidrug resistance-associated protein 1 (MRP1) inhibitory activity in the calcein AM accumulation assay and were found to be selective towards inhibition of BCRP. Substituents at position 2′ and 4′ on chalcone ring A were found to be essential for activity; additionally there was a great influence of substituents on ring B. Presence of 3,4-dimethoxy substitution on ring B was found to be optimal, while presence of 2- and 4-chloro substitution also showed a positive effect on BCRP inhibition.

Synthesis of (±)-kuwanon v and (±)-dorsterone methyl ethers via Diels-Alder reaction

The mulberry Diels-Alder adducts, the pentamethyl ethers of kuwanon V 1a and dorsterone 2a were synthesised via a biomimetic intermolecular [4+2] cycloaddition reaction between a highly electron-rich dienophile and a Lewis acid sensitive diene derived fro

Carbonylative heck reactions using CO generated ex situ in a two-chamber System

Chemical equations presented. A carbonylative Heck reaction of aryl iodides and styrene derivatives employing a two-chamber system using a stable, crystalline, and nontransition metal based carbon monoxide source is reported. By applying near-stoichiometr

The heck coupling reaction using aryl vinyl ketones: Synthesis of flavonoids

In our previous communication, an α,β-unsaturated aryl ketone was employed as the substrate olefin, which underwent arylation in the Heck coupling reaction. The use of this reagent has allowed us to design a new strategy for the synthesis of flavonoids. In this paper, we illustrate the versatility of the procedure, which was used for the preparation of several chalcones. According to our synthetic scheme, several aryl iodides, selected in order to obtain chalcones differently substituted in ring B, were treated with α,β-unsaturated ketones. All reported syntheses gave high yields. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.

Bifunctional Nanocrystalline MgO for Chiral Epoxy Ketones via Claisen-Schmidt Condensation-Asymmetric Epoxidation Reactions

Design and development of a truly nanobifunctional heterogeneous catalyst for the Claisen?Schmidt condensation (CSC) of benzaldehydes with acetophenones to yield chalcones quantitatively followed by asymmetric epoxidation (AE) to afford chiral epoxy ketones with moderate to good yields and impressive ee's is described. The nanomagnesium oxide (aerogel prepared) NAP-MgO was found to be superior over the NA-MgO and CM-MgO in terms of activity and enantioselectivity as applicable in these reactions. An elegant strategy for heterogenization of homogeneous catalysts is presented here to evolve single-site chiral catalysts for AE by a successful transfer of molecular chemistry to surface metal?organic chemistry with the retention of activity, selectivity/enantioselectivity. Bronsted hydroxyls are established as sole contributors for the epoxidation reaction, while they add on to the CSC, which is largely driven by Lewis basic O2-sites. Strong hydrogen-bond interactions between the surface ?OH on MgO and ?OH groups of diethyl tartrate are found inducing enantioselectivity in the AE reaction. Thus, the nanocrystalline NAP-MgO with its defined shape, size, and accessible OH groups allows the chemisorption of TBHP, DET, and olefin on its surface to accomplish single-site chiral catalysts to provide optimum ee's in AE reactions. Copyright