306935-95-5Relevant articles and documents
5-Aryl-furan derivatives bearing a phenylalanine- or isoleucine-derived rhodanine moiety as potential PTP1B inhibitors
Niu, Tianwei,Wang, Peipei,Li, Cheng,Dou, Tong,Piao, Huri,Li, Jia,Sun, Liangpeng
, (2020/12/04)
Two series of 5-aryl-furan derivatives bearing a phenylalanine- or isoleucine-derived rhodanine moiety were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, 5g was found to have the best PTP1B inhibitory potency (IC50 = 2.66 ± 0.16 μM) and the best cell division cycle 25 homolog B (CDC25B) inhibitory potency (IC50 = 0.25 ± 0.02 μM). Enzymatic data together with molecular modeling results demonstrated that the introduction of a sec-butyl group at the 2-position of the carboxyl group remarkably improved the PTP1B inhibitory activity.
Synthesis and antibacterial evaluation of furan derivatives bearing a rhodanine moiety
Che, Jian,Zheng, Chang-Ji,Song, Ming-Xia,Bi, Ya-Jing,Liu, Yi,Li, Yin-Jing,Wu, Yan,Sun, Liang-Peng,Piao, Hu-Ri
, p. 426 - 435 (2014/03/21)
Two series of furan derivatives bearing a rhodanine moiety (4a-l and 5a-l) have been synthesized, characterized, and evaluated for their antibacterial activity. The majority of these compounds showed potent levels of inhibitory activity against a variety of different Gram-positive bacteria, including multidrug-resistant clinical isolates, with minimum inhibitory concentration (MIC) values in the range of 2-16 μg/mL. In particular, compound 4l was found to be the most potent of the synthesized compounds against the multidrug-resistant strains, with a MIC value of 2 or 4 μg/mL. None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 at 64 μg/mL. An examination of the cytotoxicities of these agents revealed that they displayed low levels of toxicity toward HeLa cells. All of the compounds synthesized in the current paper were characterized by 1H and 13C NMR, infrared, and mass spectroscopy. Graphical Abstract: Two novel series of furan derivatives bearing a rhodanine moiety were synthesized, and evaluated for their antibacterial activity. Compounds 4l and 5a presented high potency against several multidrug-resistant clinical isolates.[Figure not available: see fulltext.]
Non-thiol farnesyltransferase inhibitors: N-(4-tolylacetylamino-3- benzoylphenyl)-3-arylfurylacrylic acid amides
Mitsch, Andreas,Wi?ner, Pia,Silber, Katrin,Haebel, Peter,Sattler, Isabel,Klebe, Gerhard,Schlitzer, Martin
, p. 4585 - 4600 (2007/10/03)
We have designed arylfurylacryl-substituted benzophenones as non-thiol farnesyltransferase inhibitors utilizing a novel aryl binding site of farnesyltransferase. These compounds display activity in the low nanomolar range. We have designed arylfurylacryl-