1369586-30-0

Upstream product

• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 52776-76-8 N-(2-pyridyl)-p-toluenesulfonamide 
• 1369585-98-7 (2S)-2-Boc-amino-1-(2-aminoimidazo[1,2-a]pyridin-3-yl)-3-phenylpropan-1-one 
• 856856-72-9 2-[2-{(p-toluenesulfonyl)imino}pyridin-1-yl]acetamide 
• 39588-26-6 2-amino-imidazo[1,2-a]pyridine 

Downstream Products

• 1369585-03-4 (4S)-4-benzyl-2-(4-nitrophenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369585-11-4 (4S)-4-benzyl-2-phenyl-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369585-14-7 (4S)-4-benzyl-2-(4-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369585-17-0 (4S)-4-benzyl-2-(3-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369585-21-6 (4S)-4-benzyl-2-(2-methylphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369585-26-1 (4S)-4-benzyl-2-(4-methoxyphenyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369585-30-7 (4S)-4-benzyl-2-isobutyl-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369585-34-1 (4S)-4-benzyl-2-(3-pyridinyl)-3,4-dihydro-5H-pyrido[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369586-22-0 (2S,4S)-4-benzyl-2-(4-nitrophenyl)-1,2,3,4-tetrahydro-5H-pyrido-[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1369586-26-4 (2R,4S)-4-benzyl-2-(4-nitrophenyl)-1,2,3,4-tetrahydro-5H-pyrido-[1',2':1,2]imidazo[4,5-d][1,3]diazepin-5-one 
• 1423171-36-1 C₂₄H₂₃N₅O₂ 

Relevant academic research and scientific papers

Pyrido-imidazodiazepinones as a new class of reversible inhibitors of human kallikrein 7

The human tissue kallikrein-7 (KLK7) is a chymotryptic serine protease member of tissue kallikrein family. KLK7 is involved in skin homeostasis and inflammation. Excess of KLK7 activity is also associated with tumor metastasis processes, especially in ovarian carcinomas, prostatic and pancreatic cancers. Development of Kallikrein 7 inhibitors is thus of great interest in oncology but also for treating skin diseases. Most of the developed synthetic inhibitors present several drawbacks such as poor selectivity and unsuitable physico-chemical properties for in vivo use. Recently, we described a practical sequence for the synthesis of imidazopyridine-fused [1,3]-diazepines. Here, we report the identification of pyrido-imidazodiazepinone core as a new potential scaffold to develop selective and competitive inhibitors of kallikrein-related peptidase 7. Structure-activity relationships (SAR), inhibition mechanisms and selectivity as well as cytotoxicity against selected cancer cell lines were investigated.

Imidazopyridine-fused [1,3]-diazepinones: Synthesis and antiproliferative activity

A series of 15 pyrido-imidazo-1,3-diazepin-5-ones and pyrido-1,3-diazepine- 2,5-diones were synthesized and their anticancer activities were evaluated. Among tested compounds on a cell lines panel, compound 6a presents the best growth inhibition activity on 21 cell lines with a cytotoxic effect on MDA-MB-435 melanoma cells. This compound led to deep cell morphological changes and revealed to be an inhibitor of the Hepatocyte progenitor kinase-like kinase (HGK), which is known to be implicated in the migration, adhesion and invasion of various tumor cells.

An efficient synthesis of pyrido-imidazodiazepinediones

We herein report the synthesis of a series of 12 optically pure 3,4-dihydro-1H-pyrido-[1′,2′:1,2]-imidazo[ 4,5-d][1,3]diazepine-2,5- diones, which form a new family of azaheterocycle-fused [1,3]diazepines. The key step of the synthesis consists in a selec

Selective C-acylation of 2-aminoimidazo[1,2- a ]pyridine: Application to the synthesis of imidazopyridine-fused [1,3]diazepinones

A series of 20 optically pure 3,4-dihydro-5H-pyrido[1′,2′:1,2] imidazo[4,5-d][1,3]diazepin-5-ones which form a new family of azaheterocycle-fused [1,3]diazepines were synthesized in four steps with 17-66% overall yields. The key step consists of a selecti