60237-54-9Relevant academic research and scientific papers
Chalcone analogue and application thereof
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Paragraph 0031-0032; 0037, (2020/07/02)
The invention discloses a chalcone analogue and application thereof, wherein the structure of the chalcone analogue is shown as a formula (I), and R is selected from substituted or unsubstituted arylor heteroaryl; the substituent groups on the aryl group
The winding road of the uvaretin class of natural products: From total synthesis to bioactive agent discovery
Dallman, Johnathan,Lansakara, Ashabha,Nguyen, Thi,Weeramange, Chamitha,Hulangamuwa, Wasundara,Rafferty, Ryan J.
, p. 1420 - 1431 (2019/08/21)
Herein, we disclose the development of a synthetic route to gain access to the uvaretin class of chalcone natural products. In this, the construction of a small library was achieved, and the collection was evaluated for cytotoxicity and other biological properties. Uvaretin (1) was accessed via a seven-step route in an overall yield of 15.1%. Within this route, the unsaturated enone variant of uvaretin (2), also a natural product, was accessed in a 16.7% yield over six steps. This route provides a nearly three-fold increase in yields of 1 and 2 in comparison to the previous synthetic route accessing them in 5.8% and 3.0% overall yields, respectively. Evaluation of 1 and 2 revealed IC50 values between 2.0 and 5.1 μM in the cancerous cell lines HeLa, U937, A549, and MIA PaCa-2. Screening of the whole chalcone library set led to the discovery of over 30 compounds, within six cancerous cell lines, possessing single digit μM IC50 activity as sole agents. Furthermore, multiple library members were found to possess promising potentiating properties with known chemotherapeutic agents.
3,5-DISUBSTITUTED PYRAZOLES USEFUL AS CHECKPOINT KINASE 1 (CHK1) INHIBITORS, AND THEIR PREPARATIONS AND APPLICATIONS
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Paragraph 000148, (2018/02/28)
Potent inhibitors of Chk1 have the structure formula (I) below. Pharmaceutical compositions comprising the Chk1 inhibitors, uses thereof and their preparation process.
Stereospecific inhibition of nitric oxide production in macrophage cells by flavanonols: Synthesis and the structure-activity relationship. Part 2
Jiang, Wen-Jun,Kitanaka, Susumu,Takamiya, Tomoko,Iijima, Hiroshi
, p. 4277 - 4284 (2017/07/22)
To explore the structure-activity relationships of flavanonols on the inhibition of nitric oxide (NO) production in RAW 264.7 cells, we have prepared a series of synthetic flavanonols. In our previous study, the 2′,3′-dihydroxyphenyl substructure was foun
ENANTIOSELECTIVE SYNTHESIS OF FLAVONOIDS. PART 1. POLY-OXYGENATED CHALCONE EPOXIDES
Augustyn, Jan A. N.,Bezuidenhoudt, Barend C. B.,Ferreira, Daneel
, p. 2651 - 2660 (2007/10/02)
Epoxidation of a series of poly-oxygenated chalcones with H2O2 in the presence of poly-α-aminoacid catalysts afforded chiral aromatic oxygenated epoxides in moderate to high optical yields; their absolute configurations were determined by CD spectroscopy.These chalcone epoxides could, in principle, be used as chirons for enantiomerically enriched dihydroflavonols.
Heterocycles. XX. Reactions of 2''-Methoxymethoxychalcone Epoxides under Acidic Conditions
Takahashi, Hiroshi,Kubota, Yumiko,Fang, Lin,Li, Shaoshun,Onda, Masayuki
, p. 4597 - 4604 (2007/10/02)
The effect of substituents on the formation of products in the reactions of 2''-methoxymethoxychalcone epoxides under acidic conditions has been examined.Regardless of the 6''-substituent, the presence of a 4'-hydroxyl group results in the exlusive format
