440348-37-8Relevant articles and documents
Synthesis and biological evaluation of asymmetric indole curcumin analogs as potential anti-inflammatory and antioxidant agents
Bandgar, Babasaheb P.,Kinkar, Santosh N.,Chavan, Hemant V.,Jalde, Shivkumar S.,Shaikh, Rafik U.,Gacche, Rajesh N.
, p. 7 - 11 (2014/03/21)
A series of asymmetric indole curcumin analogs were synthesized and evaluated as possible inhibiters of pro-inflammatory enzymes such as COX-2, pro-inflammatory cytokines as TNF-α and IL-6, trypsin and β-glucuronidase. They were also tested for antioxidant activities. The results showed that compounds 5e and 5h were found to be the most potent inhibitors of COX-2 (83.33%, 82.50%) and β-glucuronidase (67.80%, 64.12%). All the synthesized compounds exhibited promising activity against IL-6 in a range of 71-100% at 10 μM concentration. Compounds 5f, 5h, 5e, 5c and 5d showed significant inhibition against TNF-α (28-51%) and IL-6 (87-98%) with low toxicity (45-51%) against CCK-8 cells. With few exceptions, all other compounds were found to be good to excellent inhibitors of IL-6 and moderate inhibitors of TNF-α; however, the toxicity profiles of these compounds need to be ameliorated in further optimization studies. Amongst the tested compounds, 5c, 5b, 5j and 5g were found to possess excellent reducing activity and 5b, 5c and 5h were moderate DPPH (1,1-diphenyl-2-picryl hydrazine) radical scavengers.
Synthesis, biological evaluation, and molecular docking of N-{3-[3-(9-methyl-9H-carbazol-3-yl)-acryloyl]-phenyl}-benzamide/amide derivatives as xanthine oxidase and tyrosinase inhibitors
Bandgar, Babasaheb P.,Adsul, Laxman K.,Chavan, Hemant V.,Shringare, Sadanand N.,Korbad, Balaji L.,Jalde, Shivkumar S.,Lonikar, Shrikant V.,Nile, Shivraj H.,Shirfule, Amol L.
, p. 5649 - 5657 (2012/10/29)
Claisen-Schmidt condensation of 3-formyl-9-methylcarbazole with various amides of 3-aminoacetophenone afforded N-{3-[3-(9-methyl-9H-carbazol-3-yl)- acryloyl]-phenyl}-benzamide/amide derivatives. All compounds were investigated for their in vitro xanthine oxidase (XO), tyrosinase and melanin production inhibitory activity. Most of the target compounds had more potent XO inhibitory activity than the standard drug (IC50 = 4.3-5.6 μM). Interestingly, compound 7q bearing cyclopropyl ring was found to be the most potent inhibitor of XO (IC50 = 4.3 μM). Molecular modelling study gave an insight into its binding modes with XO. Compounds 7a, 7d, 7e, 7g, and 7k were found to be potent inhibitors of tyrosinase (IC50 = 14.01-17.52 μM). These results suggest the possible use of these compounds for the design and development of novel XO and tyrosinase inhibitors.
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors
Gopalsamy, Ariamala,Ciszewski, Greg,Shi, Mengxiao,Berger, Dan,Hu, Yongbo,Lee, Frederick,Feldberg, Larry,Frommer, Eileen,Kim, Steven,Collins, Karen,Wojciechowicz, Donald,Mallon, Robert
scheme or table, p. 6890 - 6892 (2010/05/19)
Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This s
