88920-24-5Relevant articles and documents
Synthesis of a new lactenediyne scaffold equipped with three handles
Banfi, Luca,Guanti, Giuseppe
, p. 7427 - 7429 (2002)
A new lactenediyne scaffold endowed with three attachment points for substituents (handles) was synthesized. This scaffold was designed in order to be used to prepare libraries of compounds possessing a tethered nucleophile, an activating substituent, and DNA-complexing substructures.
An RCM-Based Total Synthesis of the Antibiotic Disciformycin B
Altmann, Karl-Heinz,Waser, Philipp
supporting information, p. 17393 - 17397 (2020/08/14)
The total synthesis of the potent new antibiotic disciformycin B (2) is described, which shows significant activity against methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA/VRSA) strains. The synthetic route is based on macrocyclization o
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
supporting information, 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.