Synthesis and identification of novel berberine derivatives as potent inhibitors against TNF-α-induced NF-κB activation was written by Wang, Yan-Xiang;Liu, Lu;Zeng, Qing-Xuan;Fan, Tian-Yun;Jiang, Jian-Dong;Deng, Hong-Bin;Song, Dan-Qing. And the article was included in Molecules in 2017.Related Products of 777-44-6 This article mentions the following:
Twenty-three new berberine (BBR) analogs containing substituents on ring D, I [R1 = OMe, NH2, cyclopropanecarbonyloxy, (4-nitrophenyl)sulfonyloxy, etc., R2 = OMe, (adamantan-1-yl)acetoxy, (adamantane-10-carbonyloxy)], were synthesized and evaluated for their activity for suppression of tumor necrosis factor (TNF)-α-induced nuclear factor (NF)-κB activation. Structure-activity relationship (SAR) anal. indicated that suitable tertiary/quaternary carbon substitutions at the 9-position or a rigid fragment at position 10 might be beneficial for enhancing their anti-inflammatory potency. Among them, compounds I [R1 = (1-methylcyclohexane-1-carbonyl)oxy, 2-(bicyclo[2.2.1]heptan-2-yl)acetoxy, (2′-propylpentanoyl)oxy, (p-tert-butylbenzoyl)oxy, R2 = OMe] exhibited satisfactory inhibitory potency against NF-κB activation, with an inhibitory rate of around 90% (5 μM), much better than BBR. A preliminary mechanism study revealed that all of them could inhibit TNF-α-induced NF-κB activation via impairing IκB kinase (IKK) phosphorylation as well as cytokines interleukin (IL)-6 and IL-8 induced by TNF-α. Therefore, the results provided powerful information on further structural modifications and development of BBR derivatives into a new class of anti-inflammatory candidates for the treatment of inflammatory diseases. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Related Products of 777-44-6).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Related Products of 777-44-6
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics