62910-63-8Relevant articles and documents
Synthesis and antioxidant activities of berberine 9-: O -benzoic acid derivatives
Liu, Yanfei,Long, Shuo,Zhang, Shanshan,Tan, Yifu,Wang, Ting,Wu, Yuwei,Jiang, Ting,Liu, Xiaoqin,Peng, Dongming,Liu, Zhenbao
, p. 17611 - 17621 (2021/05/29)
Although berberine (BBR) shows antioxidant activity, its activity is limited. We synthesized 9-O-benzoic acid berberine derivatives, and their antioxidant activities were screened via ABTS, DPPH, HOSC and FRAP assays. The para-position was modified with halogen elements on the benzoic acid ring, which led to an enhanced antioxidant activity and the substituent on the ortho-position was found to be better than the meta-position. Compounds 8p, 8c, 8d, 8i, 8j, 8l, and especially 8p showed significantly higher antioxidant activities, which could be attributed to the electronic donating groups. All the berberine derivatives possessed proper lipophilicities. In conclusion, compound 8p is a promising antioxidant candidate with remarkable elevated antioxidant activity and moderate lipophilicity.
Synthesis of NSC 106084 and NSC 14778 and evaluation of their DNMT inhibitory activity
Leroy, Maxime,Mélin, Léa,LaPlante, Steven R.,Medina-Franco, José L.,Gagnon, Alexandre
supporting information, p. 826 - 831 (2019/01/30)
DNA methylation is an epigenetic modification that is performed by DNA methyltransferases (DNMTs) and that leads to the transfer of a methyl group from S-adenosylmethionine (SAM) to the C5 position of cytosine. This transformation results in hypermethylation and silencing of genes such as tumor suppressor genes. Aberrant DNA methylation has been associated with the development of many diseases, including cancer. Inhibition of DNMTs promotes the demethylation and reactivation of epigenetically silenced genes. NSC 106084 and 14778 have been reported to inhibit DNMTs in the micromolar range. We report herein the synthesis of NSC 106084 and 14778 and the evaluation of their DNMT inhibitory activity. Our results indicate that while commercial NSC 14778 is moderately active against DNMT1, 3A/3L and 3B/3L, resynthesized NSC 14778 is inactive under our assay conditions. Resynthesized 106084 was also found to be inactive.
Glucopyranosyl derivative and its use in medicine (by machine translation)
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Paragraph 0432; 0433; 0435; 0436, (2018/07/28)
The invention relates to a as sodium-dependent glucose transporter (SGLTs) inhibitors of the glucopyranosyl derivative, containing the pharmaceutical composition and its use in medicine, in particular of formula (I) indicated by the glucopyranosyl derivative or its pharmaceutically acceptable salt or all of its stereoisomers, or containing the pharmaceutical composition and said derivative and pharmaceutical composition for the preparation of a medicine for treating diabetes and diabetes related diseases of the use. (by machine translation)