185304-16-9

Upstream product

• 89813-47-8 N-(tert-butoxycarbonyl)-(2S,4R)-4-hydroxyproline benzyl ester 
• 80-48-8 methyl p-toluene sulfonate 
• 87691-27-8 N-tert-butoxycarbonyl-L-cis-4-hydroxyproline 
• 132622-90-3 (2S,4S)-2-benzyl 1-tert-butyl 4-hydroxypyrrolidine-1,2-dicarboxylate 
• 98-59-9 p-toluenesulfonyl chloride 
• 100-39-0 benzyl bromide 

Downstream Products

• 132622-94-7 (4R)-1-(tert-butoxycarbonyl)-4-cyano-L-proline benzyl ester 
• 185304-21-6 (2S,4R)-4-Azido-1-[2-(5-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-acetyl]-pyrrolidine-2-carboxylic acid benzyl ester 
• 185304-23-8 (2S,4R)-1-[2-(4-Amino-2-oxo-2H-pyrimidin-1-yl)-acetyl]-4-azido-pyrrolidine-2-carboxylic acid benzyl ester 
• 185304-20-5 (2S,4R)-4-Azido-1-(2-bromo-acetyl)-pyrrolidine-2-carboxylic acid benzyl ester 
• 185304-19-2 (2S,4R)-2-benzyl 1-tert-butyl 4-azidopyrrolidine-1,2-dicarboxylate 

Relevant academic research and scientific papers

NOVEL ANTIBACTERIAL CELL-PENETRATING PEPTIDES

The present disclosure relates to novel antibacterial cell-penetrating peptides and derivatives, and methods to make and use the novel antibacterial cell-penetrating peptides and derivatives. The novel antibacterial cell-penetrating peptides of the present invention with shorter linker between a pyrrolidine ring and a guanidine group provide unexpectedly higher potency against a broader scope of bacterial.

PI3K INHIBITORS AND USES THEREOF

The development of a new, targeted drug delivery paradigm coupled to improved PI3K inhibitors (e.g., PI3Kα inhibitors) represents a significant advance in cancer therapy. Provided herein are compounds, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The compounds provided herein are PI3K (e.g., PI3Kα) inhibitors and are therefore useful for the treatment and/or prevention of various diseases (e.g., proliferative diseases such as cancer). Also provided herein are nanoparticles and nanogels (e.g., P-selectin targeting nanoparticles) comprising PI3K inhibitors, such a compound described herein. In certain embodiments, a nanoparticle or nanogel described herein encapsulates a compound described herein for targeting delivery to cancer cells or tumors.

Synthesis of N(α)-(pyrinyl/pyrimidinyl acetyl)-4-aminoproline diastereomers with potential use in PNA synthesis

This paper describes an approach to introduce conformational constraint and chirality into the PNA backbone by bridging the ethylenediamine and glycine components of thesame unit by a methylene group which leads to PNA based on 4-aminoprolyl backbone with chirality at C-4 and C-2. The synthesis and characterisation of all four diasteroisomers with thymine (T) as the sidechain nucleobase (3a-d) and the synthesis of one of the stereoisomer (2S, 4R) linked to each of the four nucleobases (10-13) are described. Using these monomeric units, two model dimers (17, 18) containing four chiral centres but differing in stereochemistry at only one site were prepared and CD data on these indicate considerable structural differences in base stacking induced by chiral backbone among these.