642491-84-7

Basic information

• Product Name: 6-fluoro-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
• Synonyms: 6-fluoro-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one
• CAS NO: 642491-84-7
• Molecular Formula: C11H9FN2O
• Molecular Weight: 204.2003632
• Mol File: 642491-84-7.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 6-fluoro-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 6-fluoro-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one(642491-84-7)
• EPA Substance Registry System: 6-fluoro-2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-one(642491-84-7)

Safety Data

• Hazardous Substances Data: 642491-84-7(Hazardous Substances Data)

Upstream product

• 616-45-5 2-pyrrolidinon 
• 446-32-2 4-fluoroanthranilic acid 
• 57294-38-9 N-(tert-butoxycarbonyl)-4-aminobutanoic acid 

Relevant articles and documents

Design, Synthesis, and Evaluation of New Quinazolinone Derivatives that Inhibit Bloom Syndrome Protein (BLM) Helicase, Trigger DNA Damage at the Telomere Region, and Synergize with PARP Inhibitors

DNA damage response (DDR) pathways are crucial for the survival of cancer cells and are attractive targets for cancer therapy. Bloom syndrome protein (BLM) is a DNA helicase that performs important roles in DDR pathways. Our previous study discovered an effective new BLM inhibitor with a quinazolinone scaffold by a screening assay. Herein, to better understand the structure-activity relationship (SAR) and biological roles of the BLM inhibitor, a series of new derivatives were designed, synthesized, and evaluated based on this scaffold. Among them, compound 9h exhibited nanomolar inhibitory activity and binding affinity for BLM. 9h could effectively disrupt BLM recruitment to DNA in cells. Furthermore, 9h inhibited the proliferation of the colorectal cell line HCT116 by significantly triggering DNA damage in the telomere region and inducing apoptosis, especially in combination with a poly (ADP-ribose) polymerase (PARP) inhibitor. This result suggested a synthetic lethal effect between the BLM and PARP inhibitors in DDR pathways.

7,8,9,10-TETRAHYDRO-6H-AZEPINO, 6,7,8,9-TETRAHYDRO-PYRIDO AND 2,3-DIHYDRO-2H-PYRROLO[2,1-B]-QUINAZOLINONE DERIVATIVES

The invention relates to novel 7,8,9,10-tetrahydro-6H-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-b]-quinazolinone derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.