944906-91-6

Usage

Uses

Used in Pharmaceutical Industry:
3-PHENYL-5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZINE HYDROCHLORIDE is used as a key intermediate in the synthesis of poly(ADP-ribose)polymerase (PARP) inhibitors. These inhibitors are important in the development of targeted therapies for various types of cancer, as they can selectively kill cancer cells by exploiting their unique DNA repair mechanisms.
PARP inhibitors have shown promise in treating various types of cancer, including breast, ovarian, and pancreatic cancers. They work by inhibiting the activity of PARP enzymes, which are involved in the repair of DNA damage. By blocking the function of these enzymes, PARP inhibitors can lead to the accumulation of DNA damage in cancer cells, ultimately resulting in cell death.
In addition to their use in cancer therapy, PARP inhibitors are also being investigated for their potential applications in other therapeutic areas, such as neurodegenerative diseases and inflammatory disorders. The development of novel PARP inhibitors with improved selectivity, potency, and pharmacokinetic properties is an active area of research in the pharmaceutical industry.

Upstream product

• 1202800-41-6 C₁₉H₁₈N₄O₂ 
• 140910-71-0 8-chloro-3-phenyl-[1.2.4]triazolo[4,3-a]pyrazine 
• 1201943-50-1 3-phenyl-[1,2,4]triazolo[4,3-a]pyrazine 

Downstream Products

• 1202799-91-4 C₂₁H₁₆FN₅O₂ 
• 1202799-92-5 C₂₄H₂₁N₉O₃ 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 2,4-diaminopyrimidine derivatives as potent antitumor agents

For developing novel therapeutic agents with anticancer activities, two series of novel 2,4-diaminopyrimidine derivatives possessing triazolopiperazine or 1,4,8-triazaspiro[4.5]decan-3-one scaffolds were designed and synthesized. Preliminary investigations showed that some compounds exhibited moderate to excellent potency against four tested cancer cell lines as compared with palbociclib and momelotinib. In particular, the most promising compounds 9k and 13f showed the most potent antitumor activities with IC50 values of 2.14/1.98 μM, 3.59/2.78 μM, 5.52/4.27 μM, and 3.69/4.01 μM against A549, HCT-116, PC-3 and MCF-7 cell lines, respectively. Structure-activity relationship (SAR) studies were conducted based on the variation of the moiety of the aromatic ring and the terminal aniline on the pyrimidine core. Furthermore, the mechanism of their anticancer activity was clarified by further exploring the bioactivity. The results showed that compound 9k obviously inhibited the proliferation of A549 cell lines, induced a great decrease in the mitochondrial membrane potential leading to apoptosis of cancer cells, suppressed the migration of tumor cells and prolonged the A549 cell cycle distribution, representing blockage at the G2-M phase and accumulation at the S phase.

Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase

This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.

DIKETO AZOLOPIPERIDINES AND AZOLOPIPERAZINES AS ANTI-HIV AGENTS

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives that possess unique antiviral activity are provided. These compounds are useful the treatment of HIV and AIDS.