144432-72-4Relevant articles and documents
A new method for the synthesis of nonsymmetrical sulfamides using Burgess-type reagents
Nicolaou,Longbottom, Deborah A.,Snyder, Scott A.,Nalbanadian, Annie Z.,Huang, Xianhai
, p. 3866 - 3870 (2002)
A practical and high-yielding method for the efficient, one-step synthesis of diverse classes of N,N′-differentiated sulfamides has been developed from a wide range of amino alcohols and simple amines using Burgess-type reagents (see scheme). This method
Discovery of New Imidazo[2,1- b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising in Vitro and in Vivo Anti-melanoma Activity
Abdel-Maksoud, Mohammed S.,El-Gamal, Mohammed I.,Lee, Bong S.,Gamal El-Din, Mahmoud M.,Jeon, Hong R.,Kwon, Dow,Ammar, Usama M.,Mersal, Karim I.,Ali, Eslam M. H.,Lee, Kyung-Tae,Yoo, Kyung Ho,Han, Dong Keun,Lee, Jae Kyun,Kim, Garam,Choi, Hong Seok,Kwon, Young Jik,Lee, Kwan Hyi,Oh, Chang Hyun
, p. 6877 - 6901 (2021/06/25)
BRAF is an important component of MAPK cascade. Mutation of BRAF, in particular V600E, leads to hyperactivation of the MAPK pathway and uncontrolled cellular growth. Resistance to selective inhibitors of mutated BRAF is a major obstacle against treatment of many cancer types. In this work, a series of new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives possessing a terminal sulfonamide moiety were synthesized. Pan-RAF inhibitory effect of the new series was investigated, and structure-activity relationship is discussed. Antiproliferative activity of the target compounds was tested against the NCI-60 cell line panel. The most active compounds were further tested to obtain their IC50 values against cancer cells. Compound 27c with terminal open chain sulfonamide and 38a with a cyclic sulfamide moiety showed the highest activity in enzymatic and cellular assay, and both compounds were able to inhibit phosphorylation of MEK and ERK. Compound 38a was selected for testing its in vivo activity against melanoma. Cellular and animal activities are reported.
A kind of IDO inhibitor and use thereof
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Paragraph 0474-479, (2019/07/11)
The embodiment of the invention provides general formula (I) compound or its pharmaceutically acceptable salts, stereoisomers, a tautomeric form each other, polymorphs, solvate, prodrug, metabolite or isotope derivatives, wherein the substituents R1
Aromatic polycyclic carboxylic acid derivatives
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Paragraph 0383; 0384; 0385, (2017/08/26)
The invention specifically relates to aromatic polycyclic carboxylic acid derivative GPR40 receptor agonists as shown in a general formula (I) which is described in the specification, and pharmaceutically acceptable salts, esters or stereoisomers thereof,