66449-94-3

Upstream product

• 56-85-9 L-glutamine 
• 100-51-6 benzyl alcohol 
• 61543-21-3 (S)-benzyl 5-amino-2-((tert-butoxycarbonyl)amino)-5-oxopentanoate 
• 109396-31-8 N²-(toluene-4-sulfonyl)-L-glutamine benzyl ester 
• 23234-81-3 Z(OMe)-Gln-OH 
• 100-39-0 benzyl bromide 
• 101854-43-7 Z(OMe)-Gln-OBzl 

Downstream Products

• 104346-93-2 (S)-4-Carbamoyl-2-[(S)-2-(4-methoxy-benzyloxycarbonylamino)-4-methyl-pentanoylamino]-butyric acid benzyl ester 
• 1260170-22-6 N-(3-benzyloxycarbonyl-β-carbolin-1-yl)ethyl-L-glutamine benzyl ester 
• 1185198-32-6 N-[2-chloro-9-(tetrahydropyran-2-yl)-9H-purin-6-yl]-N-cyclopropylglycyl-L-glutamine benzyl ester 
• 1394157-72-2 benzyl N-[N'-(betulinic acid-28-oyl)-9-aminononanoyl]-L-glutaminate 
• 1184612-52-9 benzyl (S)-2-(2-(carbamoyl)ethyl)-2-(isoquinoline-3-carboxamido)acetate 
• 1219835-32-1 N-((3S)-N-(Boc-L-glutaminyl)-1,2,3,4-tetrahydroisoquinoline-3-carbonyl)-L-glutamine benzyl ester 
• 101854-36-8 Z(OMe)-Arg(Mts)-Asn-Lys(Z)-Gly-Gln-OBzl 
• 108680-70-2 Z(OMe)-Lys(Z)-His-Asn-Ile-Thr-Gln-OBzl 
• 66449-99-8 Boc-Asn-Lys(Z)-Gly-Gln-OBzl 
• 108680-68-8 Z(OMe)-Asn-Ile-Thr-Gln-OBzl 
• 101854-45-9 Z(OMe)-Lys(Z)-Gly-Gln-OBzl 
• 66450-00-8 Asn-Lys(Z)-Gly-Gln-OBzl 
• 108680-69-9 H-Asn-Ile-Thr-Gln-OBzl 
• 66449-97-6 Lys(Z)-Gly-Gln-OBzl 

Relevant academic research and scientific papers

SMALL MOLECULE DEGRADERS OF STAT3

The present disclosure provides compounds represented by Formula I or Formula VIII: wherein R1a, R1b, M, A, E, QA, and QB are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are degraders of STAT3 or dedraders of STAT3 and STAT1. Compounds of Formula VIII are inhibitors of STAT3. STAT3 degraders and inhibitors are useful for the treatment of cancer and other diseases.

A class of novel carboline intercalators: Their synthesis, in vitro anti-proliferation, in vivo anti-tumor action, and 3D QSAR analysis

Based on DOCK scores 18 N-(3-benzyloxycarbonylcarboline-1-yl)ethylamino acid benzylesters (6a-r) were synthesized as anti-tumor agents. Their IC 50 values against five human carcinoma cell lines ranged from 11.1 μM to more than 100 μM. The in vivo assay identified five derivatives of them had no anti-tumor action, the anti-tumor activity of nine derivatives of them equaled that of cytarabine, and the anti-tumor activity of three derivatives of them was higher than that of cytarabine. The UV and fluorescence spectra, as well as the relative viscosity and melting temperature measurements of calf thymus DNA (CT DNA) with and without the representative compound suggested that DNA intercalation could be their action mechanism. The 3D QSAR analysis of N-(3-benzyloxycarbonylcarboline-1-yl)ethylamino acid benzylesters (6a-r) revealed that their in vivo anti-tumor activity significantly depends on the molecular electrostatic and steric fields of the side chain of the amino acid residue.

A class of novel conjugates of substituted purine and Gly-AA-OBzl: Synthesis and evaluation of orally analgesic activity

Aimed at the chemotherapy of chronic pain two kinds of analgesic pharmacophores, substituted purine and Gly-AA-OBzl, were coupled via a five-step-reaction procedure and 19 novel conjugates N-[2-chloro-9- (tetrahydropyran-2-yl)-9H-purin-6-yl]-N-cyclopropylglycylamino acid benzylesters were provided. On mouse-tail flick model their in vivo analgesic activities were assayed. The results indicate that introducing Gly-OC2H 5 into the 6-position of the substituted purine leads to ambiguous increase of the analgesic activity, while introducing Gly-AA-OBzl into this position leads to significant increase of the analgesic activity.