802536-13-6

Basic information

• Product Name: 1H-Pyrazolo[4,3-h]quinazoline-3-carboxaMide, 4,5-dihydro-N,1-diMethyl-8-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-
• Synonyms: 1H-Pyrazolo[4,3-h]quinazoline-3-carboxaMide, 4,5-dihydro-N,1-diMethyl-8-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-;N,1-dimethyl-8-((1-(methylsulfonyl)piperidin-4-yl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;N,1-dimethyl-8-[(1-methylsulfonylpiperidin-4-yl)amino]-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide
• CAS NO: 802536-13-6
• Molecular Formula: C18H25N7O3S
• Molecular Weight: 419.5012
• Mol File: 802536-13-6.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 1H-Pyrazolo[4,3-h]quinazoline-3-carboxaMide, 4,5-dihydro-N,1-diMethyl-8-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-(CAS DataBase Reference)
• NIST Chemistry Reference: 1H-Pyrazolo[4,3-h]quinazoline-3-carboxaMide, 4,5-dihydro-N,1-diMethyl-8-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-(802536-13-6)
• EPA Substance Registry System: 1H-Pyrazolo[4,3-h]quinazoline-3-carboxaMide, 4,5-dihydro-N,1-diMethyl-8-[[1-(Methylsulfonyl)-4-piperidinyl]aMino]-(802536-13-6)

Safety Data

• Hazardous Substances Data: 802536-13-6(Hazardous Substances Data)

Usage

Explanation

This is the full chemical name of the compound, which describes its structure and components.

Explanation

The compound contains a pyrazoloquinazoline core structure, which is the central framework of the molecule.

Explanation

It is a chemical compound, which means it is a substance formed from two or more elements chemically bonded together.

Explanation

The compound acts as a potent and selective inhibitor of the enzyme PARP, which is involved in DNA repair.

Explanation

By inhibiting PARP, the compound prevents the repair of damaged DNA, leading to the death of cancer cells.

Explanation

The compound has shown potential anticancer activity in preclinical studies, making it a candidate for further investigation.

Explanation

The compound is being investigated for its potential use in treating different types of cancer due to its unique structure and mechanism of action.

Explanation

The compound's unique structure and mechanism of action make it a promising candidate for the development of new cancer therapies.

Core Structure

Pyrazoloquinazoline

Classification

Chemical Compound

Target Enzyme

Poly(ADP-ribose) polymerase (PARP)

Role in DNA Repair

Inhibition

Anticancer Activity

Promising

Cancer Treatment Potential

Various types of cancer

Development

Novel cancer therapies

Upstream product

• 218780-53-1 1-(methylsulfonyl)piperidin-4-one 

Relevant articles and documents

Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitor

Abnormal proliferation mediated by disruption of the mechanisms that keep the cell cycle under control is a hallmark of virtually all cancer cells. Compounds targeting complexes between cyclin-dependent kinases (CDKs) and cyclins (Cy) and inhibiting their activity are regarded as promising antitumor agents to complement the existing therapies. An expansion of pyrazolo[4,3-h]quinazoline chemical class oriented to the development of three points of variability was undertaken leading to a series of compounds able to inhibit CDKs both in vitro and in vivo. Starting from the CDK selective but poorly soluble hit compound 1, we succeeded in obtaining several compounds showing enhanced inhibitory activity both on CDKs and on tumor cells and displaying improved physical properties and pharmacokinetic behavior. Our study led to the identification of compound 59 as a highly potent, orally bioavailable CDK inhibitor that exhibited significant in vivo efficacy on the A2780 ovarian carcinoma xenograft model. The demonstrated mechanisms of action of compound 59 on cancer cell lines and its ability to inhibit tumor growth in vivo render this compound very interesting as potential antineoplastic agent.

PYRAZOLO-QUINAZOLINE DERIVATIVES,PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS

Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.