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Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Bharate SB,Mahajan TR,Gole YR,Nambiar M,Matan TT,Kulkarni-Almeida A,Balachandran S,Junjappa H,Balakrishnan A,Vishwakarma RA

doi

10.1016/j.bmc.2008.06.042

subject

Has Abstract

pub_date

2008-08-01 00:00:00

pages

7167-76

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)00588-9

journal_volume

16

pub_type

杂志文章

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