20093-85-0Relevant academic research and scientific papers
Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors
Taha, Muhammad,Rahim, Fazal,Ali, Muhammad,Khan, Muhammad Naseem,Alqahtani, Mohammed A.,Bamarouf, Yasser A.,Gollapalli, Mohammed,Farooq, Rai Khalid,Ali Shah, Syed Adnan,Ahmed, Qamar Uddin,Zakaria, Zainul Amiruddin
, (2019)
Chromen-4-one substituted oxadiazole analogs 1–19 have been synthesized, characterized and evaluated for β-glucuronidase inhibition. All analogs exhibited a variable degree of β-glucuronidase inhibitory activity with IC50 values ranging in betw
Synthesis of novel flavone hydrazones: In-vitro evaluation of α-glucosidase inhibition, QSAR analysis and docking studies
Imran, Syahrul,Taha, Muhammad,Ismail, Nor Hadiani,Kashif, Syed Muhammad,Rahim, Fazal,Jamil, Waqas,Hariono, Maywan,Yusuf, Muhammad,Wahab, Habibah
, p. 156 - 170 (2015)
Thirty derivatives of flavone hydrazone (5e34) had been synthesized through a five-step reaction and screened for their a-glucosidase inhibition activity. Chalcone 1 was synthesized through aldol condensation then subjected through oxidative cyclization,
Palladium-Catalyzed Chlorocarbonylation of Aryl (Pseudo)Halides Through In Situ Generation of Carbon Monoxide
Bismuto, Alessandro,Boehm, Philip,Morandi, Bill,Roediger, Sven
, p. 17887 - 17896 (2020/08/19)
An efficient palladium-catalyzed chlorocarbonylation of aryl (pseudo)halides that gives access to a wide range of carboxylic acid derivatives has been developed. The use of butyryl chloride as a combined CO and Cl source eludes the need for toxic, gaseous carbon monoxide, thus facilitating the synthesis of high-value products from readily available aryl (pseudo)halides. The combination of palladium(0), Xantphos, and an amine base is essential to promote this broadly applicable catalytic reaction. Overall, this reaction provides access to a great variety of carbonyl-containing products through in situ transformation of the generated aroyl chloride. Combined experimental and computational studies support a reaction mechanism involving in situ generation of CO.
Preparative and Regiochemical Aspects of the Palladium-Catalyzed Carbonylative Coupling of 2-Hydroxyaryl Iodides with Ethynylarenes
Ciattini, Pier Giuseppe,Morera, Enrico,Ortar, Giorgio,Rossi, Sabina Strano
, p. 6449 - 6456 (2007/10/02)
The title reaction has been conveniently carried out in DMF at 60 deg C under 1 atm CO pressure using DBU as the base and Pd(OAc)2(DPPF)2 as the catalyst to afford generally mixtures of flavones 4 and aurones 5 in varying yields, depending on the substituents in the both reactants.Factors controlling the regioselectivity for 4 or 5 formation in this and in similar, previously reported, coupling procedures have been examined.
Retinobenzoic Acids. Structure-Activity Relationships of Chalcone-4-carboxylic Acids and Flavone-4'-carboxylic Acids
Kagechika, Hiroyuki,Kawachi, Emiko,Hashimoto, Yuichi,Shudo, Koichi
, p. 834 - 840 (2007/10/02)
The structure-activity relationships of (E)-chalcone-4-carboxylic acids, which are retinoidal benzoic acids represented by R-Ph-X-Ph-COOH (4, X=-COCH=CH-), are discussed on the basis of differentiation-inducing activity on human promyelocytic leukemia cells HL-60.The activity was increased by the substitution of a bulky alkyl group(s) (R), and among such compounds, (E)-4-benzoic acid (Ch55) and (E)-4-benzoic acid (Ch80) are several times more active than retinoic acid.Though the stable conformer of chalcone derivatives is linear (s-cis form), the conformationally restricted analogue 4-(6,7,8,9-tetrahydro-6,6,9,9-tetramethyl-4H-4-oxonaphthopyran-2-yl)benzoic acid (Fv80) is more active than Ch80.While the effect of introduction of an oxygen atom varied, 4-benzoic acid (Re80), regarded as a derivative of Ch80 with two additional hydroxyl groups, has very strong activity.
