20093-85-0Relevant articles and documents
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
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.
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.