72683-79-5

Upstream product

• 67-56-1 methanol 
• 72683-77-3 N-formyl-L-m-hydroxyphenylalanine 
• 587-33-7 m-tyrosine 
• 775-06-4 D/L-3-hydroxy-phenylalanine 
• 72683-78-4 N-formyl-D-m-hydroxyphenylalanine 

Downstream Products

• 1031845-64-3 (S)-3-Benzyloxycarbonylamino-N-[(S)-2-(3-hydroxy-phenyl)-1-methoxycarbonyl-ethyl]-succinamic acid benzyl ester 
• 236393-02-5 4-(9H-fluoren-9-ylmethoxycarbonylamino)-4-[2-(3-hydroxy-phenyl)-1-methoxycarbonyl-ethylcarbamoyl]-butyric acid tert-butyl ester 
• 72683-64-8 L-aspartyl-L-m-hydroxyphenylalanine methyl ester 
• 900800-02-4 2S-tert-butoxycarbonylamino-3-(3-hydroxyphenyl)propionic acid methyl ester 
• 1263819-70-0 N-[6-(N-chlorambucilamino)hexanoyl]-L-m-tyrosine methyl ester 
• 1263819-75-5 N-[6-(N-chlorambucilamino)hexanoyl]-L-m-tyrosinol 
• 1263819-72-2 N-[11-(N-chlorambucilamino)undecanoyl]-L-m-tyrosine methyl ester 
• 1263819-81-3 N-[11-(N-chlorambucilamino)undecanoyl]-L-m-tyrosinol 
• 1263819-55-1 N-chlorambucil-L-m-tyrosine methyl ester 
• 1263819-62-0 N-chlorambucil-L-m-tyrosinol 
• 72683-65-9 L-aspartyl-D-m-hydroxyphenylalanine methyl ester 
• 959991-57-2 methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-(3-hydroxyphenyl)propanoate 
• 236393-06-9 (R)-2-{[(9S,12S,15S)-15-Acetylamino-12-(2-tert-butoxycarbonyl-ethyl)-11,14-dioxo-2-oxa-10,13-diaza-tricyclo[15.2.2.1^3,7]docosa-1⁽²⁰⁾,3⁽²²⁾,4,6,17⁽²¹⁾,18-hexaene-9-carbonyl]-amino}-3-tritylsulfanyl-propionic acid tert-butyl ester 
• 236393-03-6 (S)-4-Amino-4-[(S)-2-(3-hydroxy-phenyl)-1-methoxycarbonyl-ethylcarbamoyl]-butyric acid tert-butyl ester 

Relevant academic research and scientific papers

SMALL MOLECULE MODULATORS OF IL-17

The present invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to, to said compounds for use in therapy, to pharmaceutical compositions comprising said

CHEMICAL COMPOUNDS

The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit 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 inter alia autoinflammatory and autoimmune diseases and cancers.

SAR study of tyrosine-chlorambucil hybrid regioisomers; Synthesis and biological evaluation against breast cancer cell lines

Amino acids were transformed and coupled to chlorambucil, a well-known chemotherapeutic agent, in an attempt to create new anticancer drugs with selectivity for breast cancer cells. Among the amino acids available, tyrosine was selected to act as an estrogenic ligand. It is hypothesized that tyrosine, which shows some structural similitude with estradiol, could possibly mimic the natural hormone and, subsequently, bind to the estrogen receptor. In this exploratory study, several tyrosine-drug conjugates have been designed. Thus, ortho-, meta-and para-tyrosine-chlorambucil analogs were synthesized in order to generate new anticancer drugs with structural diversity, more specifically in regards to the phenol group location. These new analogs were produced in good yield following efficient synthetic methodology. All the tyrosine-chlorambucil hybrids were more effective than the parent drug, chlorambucil. In vitro biological evaluation on estrogen receptor positive and estrogen receptor negative (ER and ER-) breast cancer cell lines revealed an enhanced cytotoxic activity for compounds with the phenol function located at position meta. Molecular docking calculations were performed for the pure L-ortho, L-meta-and L-paratyrosine phenolic regioisomers. The synthesis of all tyrosine-chlorambucil hybrid regioisomers and their biological activity are reported herein. Possible orientations within the targeted protein [estrogen receptor alpha (ERa)] are discussed in relation to the biological activity. Springer-Verlag 2011.

ANTICANCER AGENTS BASED ON AMINO ACID DERIVATIVES

The present invention provides compounds of formula (I): in which T is L or -A-NH-C(O)-L-; L is -(CH2)n- or -(CH2)p-Z-; A is -(CH2)m- or an alkyl component of a naturally occurring amino acid; R is -CO2R1, -CH2OH, -C(O)NH(hydroxyphenyl) or C(S)NH(hydroxyphenyl); R1 is H or is C1-C12 alkyl; X is -OH, OSO2R2, -Cl, -Br, or -I; R2 is C1-C12 alkyl or -CF3; Z is phenyl or naphthyl; m is an integer having a value of 1 to 20; n is an integer having a value of 1 to 20; and p is an integer having a value of 1 to 20 or an enantiomer, diastereoisomer, racemic mixture, pharmaceutically acceptable salt, solvate or prodrug thereof. These compounds can be useful as anticancer agents.

Thiol-based angiotensin-converting enzyme 2 inhibitors: P1′ modifications for the exploration of the S1′ subsite

Explorations of the S1′ subsite of ACE2 via modifications of the P1′ methylene biphenyl moiety of thiol-based metalloprotease inhibitors led to improvements in ACE2 selectivity versus ACE and NEP, while maintaining potent ACE2 inhibi

Synthesis of two novel cyclic biphenyl ether analogs of an inhibitor of HCV NS3 protease

The synthesis of two cyclic ether analogs of a tetrapeptide inhibitor of the hepatitis C virus NS3 protease has been carried out using intramolecular nucleophilic aromatic substitution (S(N)Ar) reactions of ruthenium π-aryl complexes of pre-assembled trip

Peptide sweeteners. 4. Hydroxy and methoxy substitution of the aromatic ring in L-aspartyl-L-phenylalanine methyl ester. Structure-taste relationships.

A series of analogues of the dipeptide sweetener L-aspartyl-L-phenylalanine methyl ester having hydroxy and/or methoxy substitution on the aromatic ring was synthesized and tasted. The introduction of a methoxy group in the para position of the aromatic r