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

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

Bioorganic & medicinal chemistry (2008-07-16)
Sandip B Bharate, 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.

MATERIALS
Product Number
Brand
Product Description

Supelco
Dexamethasone, VETRANAL®, analytical standard
Sigma-Aldrich
Dexamethasone, tested according to Ph. Eur.
Sigma-Aldrich
Dexamethasone, powder, γ-irradiated, BioXtra, suitable for cell culture, ≥80% (HPLC)
Sigma-Aldrich
Dexamethasone, meets USP testing specifications
Sigma-Aldrich
Dexamethasone, powder, BioReagent, suitable for cell culture, ≥97%
Sigma-Aldrich
Dexamethasone, ≥98% (HPLC), powder