202286-29-1

Upstream product

• 521937-35-9 DL-2-(1-carboxy-1-phenylmethylaminomethylene)cyclohexane-1,3-dione 
• 2835-06-5 phenylglycin 

Downstream Products

• 1189363-92-5 7-phenyl-6,8-dihydro-5H-pyrrolo[3,4-h]quinazoline 
• 1189363-88-9 2-benzyl-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1189363-90-3 2-(4-methylbenzyl)-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1189363-91-4 2-(4-methoxybenzyl)-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1189363-87-8 2-methyl-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1575821-95-2 5-[(diethylamino)methylidene]-2-methyl-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1575821-96-3 2-benzyl-5-[(diethylamino)methylidene]-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1575821-97-4 5-[(diethylamino)methylidene]-2-(4-methylbenzyl)-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1575822-00-2 5-[(diethylamino)methylidene]-2-(4-methoxybenzyl)-1-phenyl-2,5,6,7-tetrahydro-4H-isoindol-4-one 
• 1575821-64-5 8-methyl-7-phenyl-3,5,6,8-tetrahydro-2H-pyrrolo[3,4-h]quinazolin-2-one 
• 1575821-65-6 8-benzyl-7-phenyl-3,5,6,8-tetrahydro-2H-pyrrolo[3,4-h]quinazolin-2-one 
• 1575821-66-7 8-(4-methylbenzyl)-7-phenyl-3,5,6,8-tetrahydro-2H-pyrrolo[3,4-h]quinazolin-2-one 
• 1575821-67-8 8-(4-methoxybenzyl)-7-phenyl-3,5,6,8-tetrahydro-2H-pyrrolo[3,4-h]quinazolin-2-one 
• 1575821-77-0 8-methyl-7-phenyl-6,8-dihydro-5H-pyrrolo[3,4-h]quinazolin-2-amine 

Relevant academic research and scientific papers

A facile route to pyrroles, isoindoles and hetero fused analogues

The decarboxylative cyclisation process where enamino acids derived from 1, 2-dimethylaminomethylene or 1, 2 hydroxymethylene-carbonyl compounds and amino acids gets converted into pyrroles, isoindoles and other fused pyrroles, was discussed. The cyclisat

Preclinical Activity of New [1,2]Oxazolo[5,4-e]isoindole Derivatives in Diffuse Malignant Peritoneal Mesothelioma

A series of 22 derivatives of the [1,2]oxazolo[5,4-e]isoindole system were synthesized through an efficient and versatile procedure that involves the annelation of the [1,2]oxazole moiety to the isoindole ring, producing derivatives with a wide substitution pattern. The structure-activity relationship indicates that the N-4-methoxybenzyl group appears crucial for potent activity. In addition, the presence of a 6-phenyl moiety is important and the best activity is reached with a 3,4,5-trimethoxy substituent. The most active compound, bearing both the structural features, was able to inhibit tumor cell proliferation at nanomolar concentrations when tested against the full NCI human tumor cell line panel. Interestingly, this compound was effective in reducing in vitro and in vivo cell growth, impairing cell cycle progression and inducing apoptosis, as a consequence of the inhibition of tubulin polymerization, in experimental models of diffuse malignant peritoneal mesothelioma (DMPM), a rapidly lethal disease, poorly responsive to conventional therapeutic strategies.

Synthesis of the new ring system 6,8-dihydro-5H-pyrrolo[3,4-h]quinazoline

A convenient synthesis of the pyrrolo[3,4-h]quinazoline ring system is reported. Our synthetic approach consisted of the annelation of a pyrimidine ring to an isoindole moiety using tetrahydroisoindole-4-ones as building blocks. The antiproliferative activity of the new compounds was investigated and one of them showed antitumor activity against all the 59 tested cell lines at micromolar concentrations (1.46-18.4 μM).

PYRIDYLPYRROLE COMPOUNDS USEFUL AS INTERLEUKIN-AND TNF ANTAGONISTS

The present invention provides a compound of the formula: and its pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5 and m are as defined in claim 1. The present invention also provides processes for the preparation thereof, the use thereof in treating cytokines mediated diseases and/or cell adhesion molecules (CAMs) mediated diseases and pharmaceutical compositions for use in such therapy.