- Switchable regioselection of C-H thiolation of indoles using different TMS counterions
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A switchable regioselectivity in C-H thiolation reaction by simply swapping the counteranions of TMS is reported here for the first time. An exclusive C3-H thiolation of indoles with sodium arylsulfinates was achieved in the presence of TMSCl as a promoter. In contrast, with the use of TMSOTf instead of TMSCl under otherwise identical conditions, a regiospecific C2-H thiolation of indoles was realized with the same set of substrates.
- Ji, Yuan-Zhao,Li, Hui-Jing,Zhang, Jin-Yu,Wu, Yan-Chao
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supporting information
p. 11864 - 11867
(2019/10/11)
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- Novel 2-Substituted quinolin-4-yl-benzenesulfonate derivatives: Synthesis, antiproliferative activity, and inhibition of cellular tubulin polymerization
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A series of 2-substituted quinolin-4-yl-benzenesulfonate derivatives were synthesized for the purpose of evaluating antiproliferative activity. Structure-activity relationships of the newly synthesized compounds against human lymphoblastic leukemia and va
- Kakadiya, Rajesh,Wu, Yi-Chen,Dong, Huajin,Kuo, Hsiao-Hui,Yih, Ling-Huei,Chou, Ting-Chao,Su, Tsann-Long
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scheme or table
p. 1119 - 1129
(2012/01/06)
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- CELL PROLIFERATION INHIBITORS
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Compounds having formula (I), inhibit cellular proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
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- Cell proliferation inhibitors
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Compounds having formula (I) inhibit cellular proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
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- Structure-activity relationships in platelet-activating factor (PAF). 11-From PAF-antagonism to phospholipase A2 inhibition: Syntheses and structure-activity relationships in 1-arylsulfamido-2-alkylpiperazines
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1-Benzoyl-2-alkyl piperazines are strong inhibitors of Group I and II secreted PLA2s. An improvement of their activity was obtained by replacing the amide function by a sulfamide and by introduction of electrodonor substituents on the para position of the benzenesulfonyl moiety. Neither the position on one of the carbon of the piperazine ring nor the absolute configuration of this carbon have an effect on the affinity for one or the other group of PLA2, but the lipophilicity remains for these series an essential parameter. In addition structure-activity relationships allow new hypothesis on interaction of these piperazine derivatives with the catalytic site of PLA2s.
- Binisti, Carine,Assogba, Leon,Touboul, Estera,Mounier, Carine,Huet, Jack,Ombetta, Jean-Edouard,Dong, Chang Zhi,Redeuilh, Catherine,Heymans, Francoise,Godfroid, Jean-Jacques
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p. 809 - 828
(2007/10/03)
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- Arylsulfonanilide phosphates
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The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infrections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
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