1374962-72-7

Upstream product

• 98-09-9 benzenesulfonyl chloride 
• 328-39-2 LEUCINE 
• 61-90-5 L-leucine 
• 68305-82-8 methyl (S)-4-methyl-2-(phenylsulfonamido)pentanoate 
• 2666-93-5 (S)-Leu-OMe 
• 328-38-1 (R)-leucine 
• 1738-77-8 L-leucine benzyl ester p-toluenesulfonate 
• 2743-40-0 L-leucine ethyl ester hydrochloride 
• 1370706-01-6 (S)-ethyl 4-methyl-2-(phenylsulfonamido)pentanoate 
• 1939-99-7 benzenesulfonyl chloride 

Downstream Products

• 1374962-73-8 N-benzenesulfonyl-D,L-leucyl-L-proline benzyl ester 
• 1374962-74-9 N-benzenesulfonyl-D,L-leucyl-L-proline 
• 1374962-75-0 N-benzenesulfonyl-D,L-leucyl-L-proline-[(4-cyanophenyl)methyl]amide 
• 1374962-07-8 C₂₅H₃₃N₅O₅S 
• 1374962-09-0 N-benzenesulfonyl-D,L-leucyl-L-prolyl-[(4-amidinophenyl)methyl]amide acetate 
• 1370705-88-6 (R)-4-methyl-N-((4-phenyl-1,2,5-oxadiazol-3-yl)methyl)-2-(phenylsulfonamido)pentanamide 
• 1374963-17-3 N-benzenesulfonyl-D-leucyl-L-homoproline 
• 1374962-30-7 N-benzenesulfonyl-D-leucyl-L-prolyl-{[4-(N-benzyloxycarbonyl)amidinophenyl]methyl} amide 
• 1374963-02-6 C₃₃H₃₉N₅O₆S 
• 1374963-38-8 C₂₃H₂₈N₄O₄S₂ 
• 1374963-16-2 N-benzenesulfonyl-D-leucyl-L-homoproline benzyl ester 

Relevant academic research and scientific papers

Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy

AIMP2-DX2, a splicing variant of AIMP2, is up-regulated in lung cancer, possesses oncogenic activity, and results in tumorigenesis. Specifically inhibiting the interaction between AIMP2-DX2 and HSP70 to suppress AIMP2-DX2-dependent cancers with small molecules is considered a promising avenue for cancer therapeutics. Optimization of hit BC-DXI-04 (IC50 = 40.1 μM) provided new potent sulfonamide based AIMP2-DX2 inhibitors. Among these, BC-DXI-843 showed improved inhibition against AIMP2-DX2 (IC50 = 0.92 μM) with more than 100-fold selectivity over AIMP2 in a luciferase assay. Several binding assays indicated that this compound effectively induces cancer cell apoptosis by specifically interrupting the interaction between DX2 and HSP70, which leads to the degradation of DX2 via Siah1-mediated ubiquitination. More importantly, BC-DXI-843 demonstrated in vivo efficacy in a tumor xenograft mouse model (H460 cells) at a dosage of 50 mg/kg, suggesting it as a promising lead for development of novel therapeutics targeting AIMP2-DX2 in lung cancer.

Design, synthesis, molecular docking, antimicrobial, and antioxidant activities of new phenylsulfamoyl carboxylic acids of pharmacological interest

The research explores the facile synthesis of some new phenylsulfamoyl carboxylic acids, their molecular docking, antimicrobial, and antioxidant activities. The procedure involved the mild reaction of amino acids with benzenesulfonyl chloride in a medium

New carboxamides bearing benzenesulphonamides: Synthesis, molecular docking and pharmacological properties

Ten new derivatives of benzenesulphonamide bearing carboxamide functionality were synthesized and investigated for their in vitro antimicrobial, antioxidant and in vivo anti-inflammatory activities. Compound 9d inhibited carrageenan induced rat-paw oedema

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

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

Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety

The reported toxicities of current antitrypanosomal drugs and the emergence of drug resistant trypanosomes underscore the need for the development of new antitrypanosomal agents. We report herein the synthesis and antitrypanosomal activity of 24 new amide derivatives of 3-aminoquinoline, bearing substituted benzenesulphonamide. Nine of the new derivatives showed comparable antitrypanosomal activities at IC50 range of 1–6 nM (melarsoprol 5 nM). Compound 11n and 11v are more promising antitrypanosomal agents with IC50 1.0 nM than the rest of the reported derivatives. The novel compounds showed satisfactory predicted physico-chemical properties including oral bioavailability, permeability and transport properties.

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

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

Synthesis, characterization, molecular docking and in?vitro antimalarial properties of new carboxamides bearing sulphonamide

Sulphonamides and carboxamides have shown large number of pharmacological properties against different types of diseases among which is malaria. Twenty four new carboxamide derivatives bearing benzenesulphonamoyl alkanamides were synthesized and investigated for their in silico and in?vitro antimalarial and antioxidant properties. The substituted benzenesulphonyl chlorides (1a-c) were treated with various amino acids (2a-h) to obtain the benzenesulphonamoyl alkanamides (3a-x) which were subsequently treated with benzoyl chloride to obtain the N-benzoylated derivatives (5a-f, i-n and q-v). Further reactions of the N-benzoylated derivatives or proline derivatives with 4-aminoacetophenone (6) using boric acid as a catalyst gave the sulphonamide carboxamide derivatives (7a-x) in excellent yields. The in?vitro antimalarial studies showed that all synthesized compounds had antimalarial property. Compound 7k, 7c, 7l, 7s, and 7j had mean MIC value of 0.02, 0.03, 0.05, 0.06 and 0.08?μM respectively comparable with chloroquine 0.06?μM. Compound 7c was the most potent antioxidant agent with IC50 value of 0.045?mM comparable with 0.34?mM for ascorbic acid. In addition to the successful synthesis of the target molecules using boric acid catalysis, the compounds were found to have antimalarial and antioxidant activities comparable with known antimalarial and antioxidant drugs. The class of compounds reported herein have the potential of reducing oxidative stress arising from malaria parasite and chemotherapeutic agent used in the treatment of malaria.

Evaluation of Antibacterial and Antifungal Effects of Novel Hydroxamic Acids Linked-natural Amino Acids

A SERIES of new derivatives containing hydroxamic acids linked-amino acids has been synthesized and fully characterized by spectroscopic techniques including; 1H, 13C, DEPT 135 and HRMS.These new compounds were tested for their antib

PROLINAMIDE DERIVATIVE AS THROMBIN INHIBITOR, PREPARATION METHOD AND APPLICATION THEREOF

Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.

PROLINAMIADE DERIVATIVES AS THROMBIN INHIBITOR, PREPRARATION METHOD AND APPLICATION THEREOF

Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.