6937-38-8Relevant academic research and scientific papers
Identification of novel acetylcholinesterase inhibitors: Indolopyrazoline derivatives and molecular docking studies
Chigurupati, Sridevi,Selvaraj, Manikandan,Mani, Vasudevan,Selvarajan, Kesavanarayanan Krishnan,Mohammad, Jahidul Islam,Kaveti, Balaji,Bera, Hriday,Palanimuthu, Vasanth Raj,Teh, Lay Kek,Salleh, Mohd Zaki
, p. 9 - 17 (2016)
The synthesis of novel indolopyrazoline derivatives (P1-P4 and Q1-Q4) has been characterized and evaluated as potential anti-Alzheimer agents through in vitro Acetylcholinesterase (AChE) inhibition and radical scavenging activity (antioxidant) studies. Sp
Substituted spirooxindole derivatives as potent anticancer agents through inhibition of phosphodiesterase 1
Barakat, Assem,Islam, Mohammad Shahidul,Ghawas, Hussien Mansur,Al-Majid, Abdullah Mohammed,El-Senduny, Fardous F.,Badria, Farid A.,Elshaier, Yaseen A. M. M.,Ghabbour, Hazem A.
, p. 14335 - 14346 (2018/04/27)
Spirooxindole is a promising chemo therapeutic agent. Possible targets include cancers of the liver, prostate, lung, stomach, colon, and breast. Here, we demonstrate a one-pot three-component reaction via a [3 + 2] cycloaddition/ring contraction sequence of a dipolarophile (activated alkene) with in situ-generated azomethine ylide (1,3-dipoles) without the use of any catalyst. The reaction provides efficient access to synthetically useful and biologically important spirooxindoles in high yield (69-94%) with high diastereoselectivity. The synthesized compounds were subjected to cytotoxicity evaluation using colorectal cancer (HCT-116), hepatocellular carcinoma (HepG2), and prostate cancer (PC-3) cells. Compounds 4i, 4j, and 4k showed potent cytotoxic activity and high selectivity against HCT-116 cells when compared to cisplatin. Meanwhile compound 4d retained high cytotoxic activity and selectivity against HepG2 and PC-3 cells in comparison to cisplatin. The mechanism of compound 4d was further studied using phosphodiesterase 1 enzyme and showed 74.2% inhibitory activity. A possible binding mode for compound 4d to PDE-1 was investigated by molecular modeling using OpenEye software. Pose predictions for the active compounds were demonstrated by ROCS alignments. Compound 4d has a special geometry and differs from other active compounds.
ALLOSTERIC PROTEIN KINASE MODULATORS
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Page/Page column 54, (2012/03/10)
The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
ZrCl4-mediated regio- and chemoselective friedel-crafts acylation of indole
Guchhait, Sankar K.,Kashyap, Maneesh,Kamble, Harshad
experimental part, p. 4753 - 4758 (2011/07/08)
An efficient method for regio- and chemoselective Friedel-Crafts acylation of indole using acyl chlorides in the presence of ZrCl4 has been discovered. It minimizes/eliminates common competing reactions that occur due to high and multiatom-nucleophilic character of indole. In this method, a wide range of aroyl, heteroaroyl alkenoyl, and alkanoyl chlorides undergo smooth acylation with various indoles without NH protection and afford 3-acylindoles in good to high yields.
ALLOSTERIC PROTEIN KINASE MODULATORS
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Page/Page column 112, (2010/04/30)
The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
Synthesis and antiinflammatory activity of heterocyclic indole derivatives
Rani, Preeti,Srivastava,Kumar, Ashok
, p. 449 - 452 (2007/10/03)
Chalcones of indole 1-5 and their corresponding products; pyrazolines 6-10 and azo compounds 11-15 were synthesised and evaluated for their antiinflammatory activity against carrageenan induced oedema in albino rats at a dose of 50 mg kg-1 oral
Synthesis of some new benzothia/oxazepinyl indoles as an antipsychotic agents
Bajaj, Kiran,Szivastava,Lata,Chandra, Ramesh,Kumar, Ashok
, p. 1723 - 1728 (2007/10/03)
Some new 3-(2′-substitutedaryl-2′,3′-dihydro-1′, 5′-benzothia/oxazepin-4′-yl)indoles 3a-h, 3-(2′-substitutedaryl-3′-substitutedarylaminomethylene-2′, 3′-dihydro-1′,5′-benzothia/oxazepin-4′-yl)indoles 4a-p and 3-(2′-substitutedaryl-3′-substitutedarylazo-2′
