412048-77-2

Upstream product

• 98-09-9 benzenesulfonyl chloride 
• 52488-36-5 4-bromo-1H-indole 

Downstream Products

• 460087-50-7 1-(1-Benzenesulfonyl-4-bromo-1H-indol-2-yl)-ethanone 
• 880087-00-3 tert-butyl [1-(phenylsulfonyl)-1H-indol-4-yl]acetate 
• 412048-88-5 4-(4-Methyl-1-homopiperazinyl)-1-(benzenesulfonyl)-1H-indole 
• 412048-89-6 4-(cis 3,5-Dimethyl-1-piperazinyl)-1-(benzenesulfonyl)-1H-indole 
• 1232861-11-8 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-indole 
• 880087-01-4 tert-butyl [3-nitro-1-(phenylsulfonyl)-1H-indol-4-yl]acetate 
• 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 

Relevant academic research and scientific papers

Rationally designed N-phenylsulfonylindoles as a tool for the analysis of the non-basic 5-HT6R ligands binding mode

Among all of the monoaminergic receptors, the 5-HT6R has the highest number of non-basic ligands (approximately 5% of compounds stored in 25th version of ChEMBL database have the strongest basic pKa below 5, calculated using the Instant JChem c

Construction of Oxepino[3,2-b]indoles via [4+3] Annulation of 2-Ylideneoxindoles with Crotonate-Derived Sulfur Ylides

A [4+3] annulation of 2-ylideneoxindoles with crotonate-derived sulfur ylides has been developed. A series of oxepino[3,2-b]indoles were prepared in moderate to excellent yields (62-93%) under mild conditions. Moreover, the synthetic oxepino[3,2-b] indoles can be further transformed into more complex cyclopropa[5,6]oxepino[3,2-b]indoles via a [2+1] cyclopropanation. In addition, the synthetic compounds show certain antiproliferative activity against K562 and MCF-7 cells, and its IC50 values for these two kinds of tumor cells up to 5.40±0.88 μM and 18.41±0.50 μM, respectively. (Figure presented.).

Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities

Colchicine binding site inhibitors (CBSIs) hold great potential in developing new generations of antimitotic drugs. Unlike existing tubulin inhibitors such as paclitaxel, they are generally much less susceptible to resistance caused by the overexpression

Highly diastereoselective synthesis of cyclopropane-fused spiro-pseudoindoxyl derivatives through [2 + 1] annulation of 2-ylideneoxindoles and sulfonium bromides

Compared with the intensively studied C3 spirooxindoles, limited reliable approaches are reported for synthesizing structurally analogous C2-spiropseudoindoxyl derivatives. Here, we developed an efficient method for highly diastereoselective synthesis of

Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors

A series of pyrrolo[2,3-b]pyridine-based derivatives were designed as potent Bruton's tyrosine kinase (BTK) inhibitors by using a scaffold-hopping strategy. Structure-activity relationship studies identified five compounds (3n, 3p, 3q, 3r, and 3s) with IC

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

TRICYCLIC ANILIDE HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS

Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

INDOLES AS 5-HT6 MODULATORS

The present invention relates to novel compounds of formula (I) wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for t