Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.
Тип публикации: Journal Article
Дата публикации: 2008-08-01
SCImago Q2
WOS Q1
БС1
SJR: 0.582
CiteScore: 5.6
Impact factor: 3.5
ISSN: 09680896, 14643391
PubMed ID:
18625560
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
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.
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Bharate S. et al. Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors. // Bioorganic and Medicinal Chemistry. 2008. Vol. 16. No. 15. pp. 7167-7176.
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Bharate S., Mahajan T. R., Gole Y. R., Nambiar M., Matan T. T., Kulkarni Almeida A., Balachandran S., Junjappa H., Balakrishnan A., Vishwakarma R. Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors. // Bioorganic and Medicinal Chemistry. 2008. Vol. 16. No. 15. pp. 7167-7176.
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TY - JOUR
DO - 10.1016/j.bmc.2008.06.042
UR - https://doi.org/10.1016/j.bmc.2008.06.042
TI - Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.
T2 - Bioorganic and Medicinal Chemistry
AU - Bharate, Sandip
AU - Mahajan, Tushar R
AU - Gole, Yogesh R
AU - Nambiar, Mahesh
AU - Matan, T T
AU - Kulkarni Almeida, Asha
AU - Balachandran, Sarala
AU - Junjappa, H
AU - Balakrishnan, Arun
AU - Vishwakarma, Ram
PY - 2008
DA - 2008/08/01
PB - Elsevier
SP - 7167-7176
IS - 15
VL - 16
PMID - 18625560
SN - 0968-0896
SN - 1464-3391
ER -
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BibTex (до 50 авторов)
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@article{2008_Bharate,
author = {Sandip Bharate and Tushar R Mahajan and Yogesh R Gole and Mahesh Nambiar and T T Matan and Asha Kulkarni Almeida and Sarala Balachandran and H Junjappa and Arun Balakrishnan and Ram Vishwakarma},
title = {Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors.},
journal = {Bioorganic and Medicinal Chemistry},
year = {2008},
volume = {16},
publisher = {Elsevier},
month = {aug},
url = {https://doi.org/10.1016/j.bmc.2008.06.042},
number = {15},
pages = {7167--7176},
doi = {10.1016/j.bmc.2008.06.042}
}
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MLA
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Bharate, Sandip, et al. “Synthesis and evaluation of pyrazolo[3,4-b]pyridines and its structural analogues as TNF-alpha and IL-6 inhibitors..” Bioorganic and Medicinal Chemistry, vol. 16, no. 15, Aug. 2008, pp. 7167-7176. https://doi.org/10.1016/j.bmc.2008.06.042.
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