Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents
Publication type: Journal Article
Publication date: 2011-03-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
21345672
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Stellatin (4), isolated from Dysophylla stellata is a cyclooxygenase (COX) inhibitor. The present study reports the synthesis and biological evaluation of new stellatin derivatives for COX-1, COX-2 inhibitory and anti-inflammatory activities. Eight derivatives showed more pronounced COX-2 inhibition than stellatin and, 17 and 21 exhibited the highest COX-2 inhibition. They also exhibited the significant anti-inflammatory activity in TPA-induced mouse ear edema assay and their anti-inflammatory effects were more than that of stellatin and indomethacin at 0.5mg/ear. The derivatives were further evaluated for antioxidant activity wherein 16 and 17 showed potent free radical scavenging activity against DPPH and ABTS radicals. Molecular docking study revealed the binding orientations of stellatin and its derivatives into the active sites of COX-1 and COX-2 and thereby helps to design the potent inhibitors.
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65
Total citations:
65
Citations from 2024:
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(10.77%)
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GOST
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Gautam R. et al. Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 6. pp. 1612-1616.
GOST all authors (up to 50)
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Gautam R., Jachak S. M., Kumar V., Mohan C. G. Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 6. pp. 1612-1616.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.bmcl.2011.01.116
UR - https://doi.org/10.1016/j.bmcl.2011.01.116
TI - Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Gautam, Raju
AU - Jachak, Sanjay M.
AU - Kumar, Vivek
AU - Mohan, Chethampadi Gopi
PY - 2011
DA - 2011/03/01
PB - Elsevier
SP - 1612-1616
IS - 6
VL - 21
PMID - 21345672
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
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@article{2011_Gautam,
author = {Raju Gautam and Sanjay M. Jachak and Vivek Kumar and Chethampadi Gopi Mohan},
title = {Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2011},
volume = {21},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.bmcl.2011.01.116},
number = {6},
pages = {1612--1616},
doi = {10.1016/j.bmcl.2011.01.116}
}
Cite this
MLA
Copy
Gautam, Raju, et al. “Synthesis, biological evaluation and molecular docking studies of stellatin derivatives as cyclooxygenase (COX-1, COX-2) inhibitors and anti-inflammatory agents.” Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 6, Mar. 2011, pp. 1612-1616. https://doi.org/10.1016/j.bmcl.2011.01.116.