| Literature DB >> 18625560 |
Sandip B Bharate1, Tushar R Mahajan, Yogesh R Gole, Mahesh Nambiar, T T Matan, Asha Kulkarni-Almeida, Sarala Balachandran, H Junjappa, Arun Balakrishnan, Ram A Vishwakarma.
Abstract
In the present article, we have synthesized three different series of pyrazolo[3,4-b]pyridines and their structural analogues using novel synthetic strategy involving one-pot condensation of 5,6-dihydro-4H-pyran-3-carbaldehyde/2-formyl-3,4,6-tri-O-methyl-D-glucal/chromone-3-carbaldehyde with heteroaromatic amines. All synthesized compounds were evaluated for their anti-inflammatory activity against TNF-alpha and IL-6. Out of 28 compounds screened, 40, 51, 52 and 56 exhibited promising activity against IL-6 with 60-65% inhibition at 10 microM concentration. Amongst these, 51, 52 and 56 showed potent IL-6 inhibitory activity with IC(50)'s of 0.2, 0.3 and 0.16 microM, respectively. Compound 56 was not cytotoxic in CCK-8 cells up to the concentration of >100 microM.Entities:
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Year: 2008 PMID： 18625560 DOI： 10.1016/j.bmc.2008.06.042
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641