75158-60-0Relevant academic research and scientific papers
Exploration of benzofuran-based compounds as potent and selective Plasmodium falciparum glycogen synthase kinase-3 (PfGSK-3) inhibitors
Moolman, Chantalle,van der Sluis, Rencia,Beteck, Richard M.,Legoabe, Lesetja J.
, (2021/04/09)
Plasmodium falciparum glycogen synthase kinase-3 (PfGSK-3) has been identified as a potential target for the development of novel drugs against multi-drug resistant malaria. A series of benzofuran-based compounds was synthesised and evaluated as inhibitors of recombinantly expressed and purified PfGSK-3 and human glycogen synthase kinase-3 beta (HsGSK-3β). Of this series, five compounds (5k, 5m, 5p, 5r, 5s) preferentially inhibited PfGSK-3, with four of these compounds exhibiting IC50 values in the sub-micromolar range (0.00048–0.440 μM). Evaluation of the structure-activity relationships required for PfGSK-3 selective inhibition indicated that a C6-OCH3 substitution on ring A is preferred, while the effect of the ring B substituent on activity, in decreasing order is: C4′-CN > C4′-F > C3′-OCH3 > C3′,4′-diCl. To date, development of PfGSK-3 inhibitors has been limited to the 4-phenylthieno[2,3-b]pyridine class. Chalcone-based scaffolds, such as the benzofurans described herein, are promising new hits which can be explored for future design of PfGSK-3 selective inhibitors.
Syntheses of 2-Aroyl Benzofurans through Cascade Annulation on Arynes
Gouthami, Pashikanti,Chavan, Lahu N.,Chegondi, Rambabu,Chandrasekhar, Srivari
, p. 3325 - 3332 (2018/03/25)
The highly efficient and expedient route for the syntheses of 2-aroyl benzofurans has been developed via the cascade [2+2] followed by a [4+1] annulation on arynes. The overall transformation proceeded through the formation of ortho-quinone methide by the
DABCO-promoted efficient and convenient synthesis of benzofurans
Meshram,Reddy, B. Chennakesava,Prasad,Goud, P. Ramesh,Kumar, G. Santosh,Kumar, R. Naveen
experimental part, p. 1669 - 1676 (2012/05/04)
An efficient and convenient synthesis of benzofurans has been described from phenacyl halides and o-hydroxy benzaldehyde in the presence of DABCO. The procedure is applicable for a variety of phenacyl halides and provide a variety of benzofurans. DABCO ac
Potent CYP19 (aromatase) 1-(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: Synthesis and biological evaluation
Saberi, Mohammed Reza,Vinh, Tai Ky,Yee, Sook Wah,Griffiths, B. J. Nathan,Evans, Peter J.,Simons, Claire
, p. 1016 - 1022 (2007/10/03)
The synthesis of a series of novel 1-[(benzofuran-2-yl)phenylmethyl]- pyridine, -imidazole, and -triazole derivatives is described. All the compounds were evaluated in vitro for inhibitory activity against aromatase (P450 AROM, CYP19), using hu
BENZOFURAN DERIVATIVES, FORMULATIONS AND USES THEREOF
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Page 16-17, (2010/02/06)
The present invention is concerned with benzofuran derivatives, pharmaceutical formulations and products containing the same, and uses thereof. More particularly, there is disclosed a compound of formula (I), or a pharmaceutically acceptable salt, or prod
The Reduction of 2-Benzylidene-3(2H)-benzofuranones with Lithium Aluminium Hydride-Aluminium Chloride
Kurosawa, Kazu,Morita, Yasuhiro
, p. 635 - 636 (2007/10/02)
The reduction of various 2-benzylidene-3(2H)-benzofuranones with lithium aluminium hydride-aluminium chloride in ether gave the corresponding 2-benzylbenzofurans in moderate yields.The reduction of 6-methoxy-2-(4-methoxybenzoyl)benzofuran also yielded 6-m
The Reactions of 2-Phenyl-2H-1-benzopyrans and 2-Phenyl-4H-1-benzopyrans with Lead(IV) Acetate
Kurosawa, Kazu,Yamaguchi, Katsutoshi,Nagata, Yasuyuki,Ohki, Hisatake
, p. 1769 - 1770 (2007/10/02)
The reactions of 7-methoxy-2-phenyl-2H-1-benzopyran and 7-methoxy-2-phenyl-4H-1-benzopyran with lead(IV) acetate gave 2-benzoyl-6-methoxybenzofuran and 6-acetoxy-3-methoxy-6-(3-oxo-3-phenyl-1-propenyl)-2,4-cyclohexadien-1-one.The reactions of 7-methoxy-2-
