Structure-activity relationship of aloperine derivatives as new anti-liver fibrogenic agents was written by Wang, Kun;Guo, Zhihao;Bao, Yunyang;Pang, Yudong;Li, Yinghong;He, Hongwei;Song, Danqing. And the article was included in Molecules in 2020.Recommanded Product: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride This article mentions the following:
Novel 12N-substituted aloperine derivatives I [R = Et, 3,4,5-trimethylphenyl, oxan-4-yl, etc.; R1 = H, Me, naphthalen-2-yl; RR1 = -(CH2)4-] and 12N-N’-phenoxazinylcarbamoylmethyl aloperine, II [R2 = naphthalen-1-yl, 3-(trifluoromethyl)phenyl, Ph, 4-bromo-3-(trifluoromethyl)phenyl], III [R2 = Bu, 3-(trifluoromethoxy)phenyl, 3-bromophenyl, etc.]were synthesized and investigated for their inhibitory effects on collagen α1 (I) (COL1A1) promotor in human hepatic stellate LX-2 cells, taking aloperine (1) as the hit. A structure-activity relationship (SAR) study disclosed that the introduction of suitable substituents on the 12N atom might enhance the activity. Compound 12N-N’-phenoxazinylcarbamoylmethyl aloperine exhibited a good promise on down-regulating COL1A1 expression with the IC50 value of 16.5μM. Its inhibitory activity against COL1A1 was further confirmed on both mRNA and protein levels. Meanwhile, it effectively inhibited the expression of other fibrogenic proteins, such as transforming growth factor β1 (TGF-α1) and smooth muscle actin (α-SMA). It also exhibited good in vivo safety profile with the oral LD50 value of 400 mg kg-1 in mice. The results initiated the anti-liver fibrogenic study of aloperine derivatives, and the key compound 12N-N’-phenoxazinylcarbamoylmethyl aloperine was selected as a novel lead for further investigation against liver fibrogenesis. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Recommanded Product: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Recommanded Product: 3-(Trifluoromethyl)benzene-1-sulfonyl chloride
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics