1232861-11-8

Basic information

• Product Name: 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-indole
• Synonyms: 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-indole
• CAS NO: 1232861-11-8
• Molecular Weight: 350.236
• Mol File: 1232861-11-8.mol

Chemical Properties

• CAS DataBase Reference: 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-indole(CAS DataBase Reference)
• NIST Chemistry Reference: 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-indole(1232861-11-8)
• EPA Substance Registry System: 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-indole(1232861-11-8)

Safety Data

• Hazardous Substances Data: 1232861-11-8(Hazardous Substances Data)

Upstream product

• 74-88-4 methyl iodide 
• 412048-77-2 1‐(benzenesulfonyl)‐4‐bromo‐1H‐indole 
• 52488-36-5 4-bromo-1H-indole 
• 98-09-9 benzenesulfonyl chloride 

Downstream Products

• 6127-18-0 4-bromo-2-methyl-1H-indole 
• 34058-51-0 methyl 2-methyl-1H-indole-4-carboxylate 
• 1542706-34-2 1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxylic acid 
• 1542706-15-9 1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-N,2-dimethyl-1H-indole-4-carboxamide 
• 1542711-68-1 methyl 1-(4-(benzylamino)-5,6,7,8-tetrahydroquinazolin-2-yl)-2-methyl-1H-indole-4-carboxylate 
• 1542706-36-4 1-(4-(benzylamino)-5,6,7,8-tetrahydroquinazolin-2-yl)-2-methyl-1H-indole-4-carboxylic acid 
• 1542705-09-8 1-(4-(benzylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carbonitrile 
• 1542705-83-8 1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carbonitrile 
• 1542705-59-8 1-[4-(benzylamino)-5,6,7,8-tetrahydroquinazolin-2-yl]-2-methyl-1H-indole-4-carbonitrile 
• 1542706-02-4 1-(4-(benzylamino)-5,6,7,8-tetrahydroquinazolin-2-yl)-2-methyl-1H-indole-4-carboxamide 
• 1542705-58-7 1-(4-(benzylamino)-5,6,7,8-tetrahydropyrido[4,3-d]-pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide 
• 1360883-22-2 2-methyl-1H-indole-4-carbonitrile 

Relevant articles and documents

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

The AAA-ATPase p97 plays vital roles in mechanisms of protein homeostasis, including ubiquitin-proteasome system (UPS) mediated protein degradation, endoplasmic reticulum-associated degradation (ERAD), and autophagy. Herein we describe our lead optimization efforts focused on in vitro potency, ADME, and pharmaceutical properties that led to the discovery of a potent, ATP-competitive, D2-selective, and orally bioavailable p97 inhibitor 71, CB-5083. Treatment of tumor cells with 71 leads to significant accumulation of markers associated with inhibition of UPS and ERAD functions, which induces irresolvable proteotoxic stress and cell death. In tumor bearing mice, oral administration of 71 causes rapid accumulation of markers of the unfolded protein response (UPR) and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. 71 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors.

FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX

Fused pyrimidine compounds having a saturated, unsaturated or aromatic A ring fused to a pyrimidine ring and having a complex substituents at the 2 position and a substituted amine at the 4 position of the pyrimidine ring as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine ring and A ring are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.

ETHYNYLINDOLE COMPOUNDS

As a compound having a potent oral activity and a long-lasting cysLT1/cysLT2 receptor antagonistic activity, the compound of the formula (I): which exhibits potent antagonistic activity against the cysLT1/cysLT2 /sub