134307-72-5

Upstream product

• 77987-49-6 benzyl 2-hydroxyethylcarbamate 
• 124-63-0 methanesulfonyl chloride 
• 141-43-5 ethanolamine 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 134307-73-6 <1-¹³C>-3-Benzyloxycarbonylaminopropionitrile 
• 595544-64-2 2-{4-[2-(2-Oxo-2-pyrrolidin-1-yl-ethyl)-2H-pyrazol-3-yl]-phenoxy)-ethyl-carbamic Acid Benzyl Ester 
• 595544-49-3 (2-{4-[2-(2-Oxo-2-pyrrolidin-1-ylethyl)-oxazol-4-yl]-phenoxy}-ethyl)-carbamic Acid Benzyl Ester 
• 3560-45-0 benzyl-{2-[(2-hydroxyethyl)amino]ethyl}carbamate 
• 1128238-20-9 N-(2-(4-cyanophenoxy)ethyl)-2-phenylacetamide 
• 1095422-54-0 benzyl 2-(2-bromo-5-iodophenoxy)ethylcarbamate 
• 1095422-73-3 N-{2-[5'-cyano-2'-(2-phenylacetylamino-ethoxy)-biphenyl-3-yloxy]-ethyl}-2-phenyl-acetamide 
• 1128237-29-5 dibenzyl 2,2'-(3-bromo-6-iodo-1,2-phenylene)bis(oxy)bis(ethane-2,1-diyl)dicarbamate 
• 1095422-56-2 dibenzyl 2,2'-(4-cyanobiphenyl-2,2'-diyl)bis(oxy)bis(ethane-2,1-diyl)dicarbamate 
• 1095422-58-4 dibenzyl 2,2'-(4-cyanobiphenyl-2,3'-diyl)bis(oxy)bis(ethane-2,1-diyl)dicarbamate 
• 1095422-60-8 dibenzyl 2,2'-(4-bromobiphenyl-3,2'-diyl)bis(oxy)bis(ethane-2,1-diyl)dicarbamate 
• 1095422-63-1 dibenzyl 2,2'-(4-bromobiphenyl-3,3'-diyl)bis(oxy)bis(ethane-2,1-diyl)dicarbamate 
• 1095422-69-7 dibenzyl 2,2'-(5-cyanobiphenyl-2,2'-diylbis(oxy))bis(ethane-2,1-diyl)tetracarbamate 
• 1095422-53-9 dibenzyl 2,2'-(3-bromo-1,2-phenylene)bis(oxy)bis(ethane-2,1-diyl)dicarbamate 

Relevant academic research and scientific papers

Discovery of New Imidazo[2,1- b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising in Vitro and in Vivo Anti-melanoma Activity

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.

Design, synthesis and anticancer profile of new 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-linked sulfonamide derivatives with V600EBRAF inhibitory effect

A new series of 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine linked sulfonamide derivatives 12a–n was designed and synthesized according to the structure of well-established V600EBRAF inhibitors. The terminal sulfonamide moiety was linked to the pyrimidine ring via either ethylamine or propylamine bridge. The designed series was tested at fixed concentration (1 μM) against V600EBRAF, finding that 12e, 12i and 12l exhibited the strongest inhibitory activity among all target compounds and 12l had the lowest IC50 of 0.49 μM. They were further screened on NCI 60 cancer cell lines to reveal that 12e showed the most significant growth inhibition against multiple cancer cell lines. Therefore, cell cycle analysis of 12e was conducted to investigate the effect on cell cycle progression. Finally, virtual docking studies was performed to gain insights for the plausible binding modes of vemurafenib, 12i, 12e and 12l.

Anticancer profile and anti-inflammatory effect of new N-(2-((4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine sulfonamide derivatives

A new series of N-(2-((4-(1,3-diphenyl-1H-pyrazol-4-yl)pyridine sulfonamide derivatives 11a-o were designed and synthesized based on our previous works. The new series was tested for its anticancer and anti-inflammatory effects. The anticancer profile of

Solution-Phase Synthesis of Backbone-Constrained Cationic Peptoid Hexamers with Antibacterial and Anti-Biofilm Activities

Abstract: Submonomer synthesis in solution and block-coupling protocols were combined to prepare amphiphilic peptoid hexamers. The amphipathic character arises from the use of hydrophobic aliphatic tert-butyl side-chains imposing the cis-amide backbone co

SULFONAMIDE DERIVATIVES AND USES THEREOF

The present disclosure relates to compounds of Formula (I) or (II): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.

Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies

A series of imidazothiazole derivatives possessing potential activity against melanoma cells were investigated for molecular mechanism of action. The target compounds were tested against V600E-B-RAF and RAF1 kinases. Compound 1zb is the most potent agains

Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF

Several pyrrolo[2,3-b]pyridine-based B-RAF inhibitors are well known and some of them are currently FDA approved as anticancer agents. Based on the structure of these FDA approved V600EB-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold were designed and synthesized in attempt to develop new potent V600EB-RAF inhibitors. The 38 synthesized compounds were biologically evaluated for their V600EB-RAF inhibitory effect at single dose (10 μM). Compounds with high percent inhibition were tested to determine their IC50 over V600EB-RAF. Compounds 34e and 35 showed the highest inhibitory effect with IC50 values of 0.085 μM and 0.080 μM, respectively. Headed for excessive biological evaluation, the synthesized derivatives were tested over sixty diverse human cancer cell lines. Only compound 35 emerged as a potent cytotoxic agent against different panel of human cancer cell lines.

IRAK DEGRADERS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

Broad-spectrum antiproliferative activity of a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives

This article described the synthesis and in vitro antiproliferative activities a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives. The nine target compounds were tested for in vitro antitumor effect against a

Design, synthesis, and in vitro antiproliferative and kinase inhibitory effects of pyrimidinylpyrazole derivatives terminating with arylsulfonamido or cyclic sulfamide substituents

A novel series of substituted pyrimidine compounds bearing N-phenylpyrazole and terminating with aryl and cyclic sulfonamido moiety were designed, synthesized, and evaluated in vitro as antiproliferative agents against a panel of 53 cell lines of differen