136833-36-8Relevant articles and documents
Quinazolinone compounds antagonizing NODDDD1/2 receptor signaling pathway
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Paragraph 0303-0305; 0342-0347, (2021/09/08)
I II Of the compounds are capable of being used for immunotherapy of organisms by antagonizing NODDDD1/2 signaling pathway activation, and in particular can be used for treating tumors, and belongs to the technical field of medicines and.
Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy
Ma, Yao,Yang, Jingshu,Wei, Xiduan,Pei, Yameng,Ye, Jingjia,Li, Xueyuan,Si, Guangxu,Tian, Jingyuan,Dong, Yi,Liu, Gang
, (2020/09/15)
Nucleotide-binding oligomerization domain-containing protein 1 and 2 (NOD1/2) receptors are potential immune checkpoints. In this article, a quinazolinone derivative (36b) as a NOD1/2 dual antagonist was identified that significantly sensitizes B16 tumor-bearing mice to paclitaxel treatment by inhibiting both nuclear factor κB (NF-κB) and mitogen-activated protein kinase inflammatory signaling that mediated by NOD1/2.
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
Wang, Suhua,Yang, Jingshu,Li, Xueyuan,Liu, Zijie,Wu, Youzhen,Si, Guangxu,Tao, Yiran,Zhao, Nan,Hu, Xiao,Ma, Yao,Liu, Gang
, p. 5162 - 5192 (2017/06/28)
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.
Substituted benzodiazepine ring compound and preparation method and application thereof
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Paragraph 0304-0306, (2017/07/22)
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.
Compound and application thereof
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Paragraph 0193, (2016/10/09)
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
Wu, Hao,Xie, Xilei,Liu, Gang
experimental part, p. 346 - 355 (2010/10/18)
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.
AMINOALYL-IMIDAZOTETRAZINES FOR TREATMENT OF CANCER
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Page/Page column 38, (2009/12/02)
The present invention relates to imidazotetrazines of Formula (I) and their use in the treatment of cancer.
VIRAL POLYMERASE INHIBITORS
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Page/Page column 76-77, (2008/06/13)
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein either A or B is nitrogen and the other B or A is C, and the radicals R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particularly those viral polymerases within the Flaviviridae family, more particularly to HCV polymerase.
N-3-substituted imidazoquinazolinones: Potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction
Rotella, David P.,Sun, Zhong,Zhu, Yeheng,Krupinski, John,Pongrac, Ronald,Seliger, Laurie,Normandin, Diane,Macor, John E.
, p. 1257 - 1263 (2007/10/03)
Phosphodiesterase type 5 (PDE5) inhibitors with improved PDE isozyme selectivity relative to sildenafil may result in agents for the treatment of male erectile dysfunction (MED) with a lower incidence of PDE-associated adverse effects. This paper describe
Quinazolinone inhibitors of cGMP phosphodiesterase
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, (2008/06/13)
Novel quinazolinone compounds, methods of using such compounds in the treatment of cGMP-associated conditions such as erectile dysfunction, and pharmaceutical compositions containing such compounds.