140373-38-2

Upstream product

• 5678-47-7 3-amino-3-(3-nitro-phenyl)-propionic acid 
• 158325-90-7 3-Amino-3-(3-nitrophenyl)propionamide 
• 67-56-1 methanol 
• 99-61-6 3-nitro-benzaldehyde 

Downstream Products

• 1257211-85-0 (R)-1-[3-benzamido-3-(3-nitrophenyl)propanamido]-3-methylbutylboronic acid 
• 640238-28-4 3-benzamido-3-(3-nitrophenyl)propanoic acid 
• 1269634-20-9 C₁₇H₁₆N₂O₅ 

Relevant academic research and scientific papers

Synthesis and biological evaluation of 3-phenyl-3-aryl carboxamido propanoic acid derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26A1)

All-trans-retinoic acid (ATRA), the biologically active metabolite of vitamin A, is used medicinally for the treatment of hyperproliferative diseases and cancers. However, it is easily metabolized. In this study, the leading compound S8 was found based on virtual screening. To improve the activity of the leading compound S8, a series of novel S8 derivatives were designed, synthesized and evaluated for their in vitro biological activities. All of the prepared compounds showed that substituting the 5-chloro-3-methyl-1-phenyl-1H-pyrazole group for the 2-tertbutyl-5-methylfuran scaffold led to a clear increase in the biological activity. The most promising compound 32, with a CYP26A1 IC50 value of 1.36 μM (compared to liarozole (IC50 = 2.45 μM) and S8 (IC50 = 3.21 μM)) displayed strong inhibitory and differentiation activity against HL60 cells. In addition, the study focused on the effect of β-phenylalanine, which forms the coordination bond with the heme of CYP26A1. These studies suggest that the compound 32 can be used as an appropriate candidate for future development.

Synthesis, in vitro and in vivo biological evaluation, and comprehensive understanding of structure-activity relationships of dipeptidyl boronic acid proteasome inhibitors constructed from β-amino acids

An extensive structure-activity relationship (SAR) study of 72 dipeptidyl boronic acid proteasome inhibitors constructed fromβ -amino acids is reported. SAR analysis revealed that bicyclic groups at the R1 position, 3-F substituents at the Rsu

Benzodiazepine cholecystokinin antagonists

Benzodiazepine analogs of the formula: STR1 are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Anti-tumor compounds

The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: STR1 wherein R1 includes hydrogen, amino and alkyl or alkoxy each of up to 4 carbon atoms; R2 includes hydrogen, alkyl, hydroxyalkyl and halogenoalkyl each of up to 4 carbon atoms; R3 is hydrogen or alkyl or up to 3 carbon atoms; Ar is phenylene or heterocyclene; L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR4 --, --NR4.CO--, --CH=CH-- or --CO.O--, wherein R4 is alkyl of up to 4 carbon atoms; and Y is a branched alkyl group bearing substituents Y2 and Y3 the definition of each independently including hydroxy, cyano, aryl and heteroaryl, and the definition of Y3 also optionally including sulpho, N-phenylsulphonylcarbamoyl and 5-tetrazolyl; or a pharmaceutically-acceptable salt thereof.