408339-11-7

Upstream product

• 67-56-1 methanol 
• 29235-52-7 2,4,5-trinitro-benzoic acid 
• 455-38-9 3-fluorobenzoic acid 
• 591-31-1 3-methoxy-benzaldehyde 
• 535-80-8 3-chlorobenzoate 
• 136833-36-8 5-chloro-2,4-dinitrobenzoic acid 
• 80410-57-7 3-methoxy-4-nitrobenzaldehyde 
• 51676-74-5 1-chloro-5-methyl-2,4-dinitrobenzene 
• 20357-24-8 5-methoxy-2-nitro-benzaldehyde 
• 393-93-1 5-fluoro-2,4-dinitro-benzoic acid 
• 860243-67-0 5-methoxy-2,4-dinitrobenzaldehyde 

Relevant academic research and scientific papers

Substituted benzodiazepine ring compound and preparation method and application thereof

The invention discloses a substituted benzodiazepine ring compound and a preparation method and application thereof and further relates to a pharmaceutical composition and application of the compound. According to the substituted benzodiazepine ring compound, the effect of preventing or treating an immune inflammatory disease or tumor is achieved through activation of a selectively antagonistic or collaboratively excited NOD1/2 signal transduction pathway; the substituted benzodiazepine ring compound has a polypeptidase stability and is not degraded by polypeptidase in the organism.

Discovery of 1,4-Benzodiazepine-2,5-dione (BZD) Derivatives as Dual Nucleotide Binding Oligomerization Domain Containing 1/2 (NOD1/NOD2) Antagonists Sensitizing Paclitaxel (PTX) to Suppress Lewis Lung Carcinoma (LLC) Growth in Vivo

Nucleotide-binding oligomerization domain-like receptors (NLRs) are intracellular sensors of pathogen-Associated molecular patterns (PAMPs) and damage-Associated molecular patterns (DAMPs). Previously, we reported nucleotide-binding oligomerization domain-containing protein 1 (NOD1) antagonists (11, 12) and a NOD2 antagonist (9) that sensitized docetaxel (DTX) or paclitaxel (PTX) treatment for breast or lung cancer. In this article, we describe for the first time a 1,4-benzodiazepine-2,5-dione (BZD) derivative (26bh) that acts as a dual NOD1/NOD2 antagonist and inhibits both nuclear factor B (NF-B) and mitogen-Activated protein kinase (MAPK) inflammatory signaling, thereby sensitizing PTX to suppress Lewis lung carcinoma (LLC) growth. After investigation of the compound's cytotoxicity, a systematic structure-Activity relationship (SAR) was completed and revealed several key factors that were necessary to maintain antagonistic ability. This study establishes the possibility for using adjuvant treatment to combat cancer by antagonizing both NOD1 and NOD2 signaling.

Compound and application thereof

The invention discloses a compound and application thereof. The compound is the compound shown in the formula (I) or a stereoisomer or a pharmaceutical acceptable salt or solvate or a prodrug of the compound shown in the formula (I). The compound can restrain tumor cell proliferation through the effect RRM2, and restrain tumor stem cell regeneration, thereby being effectively used for preparing medicine for preventing or treating proliferative diseases and particularly anti-cancer medicine.

Parallel solution phase synthesis of 3,6,7-4(3 H)-Quinazolinones and evaluation of their antitumor activities against human cancer

Three diversity points of 4(3H)-quinazolinone are introduced at the 3-, 6-, and 7-positions with an efficient parallel solution-phase synthetic method. A one-pot synthesis was developed that gave the key intermediate in high yield. Five hit compounds exhibit preferable activities against a panel of human tumor cell lines, which pointed out preliminary structure-activity relationships.