Zn‐Phenanthroline‐Dicarboxylate Complex: A Dual Inhibitor of COX‐2 and 5‐LOX Enzymes

Darsi Rambabu;Sharma, Shilpa;Mayank;Singh, Narinder;Pooja;et.al.
(2024) ChemistrySelect — Vol. 9, n° 23, p. e202400310 (2024)

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Authors
  • Darsi Rambabuorcid-logoUCLouvain
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  • Sharma, Shilpa
    Author
  • Mayank
    Author
  • Singh, Narinder
    Author
  • Poojaorcid-logo
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Abstract
A series of new phenanthroline-based metal complexes, coordination polymers are synthesized using 1,10-phenanthroline 2,9-dicarboxylate (PDA) and different metal salts including tin (R-1 to R-3), manganese (R-4), ruthenium (R-5), and zinc (R-6) respectively. The inhibitory activities of synthesized coordination compounds are evaluated towards COX-2 (cyclooxygenase-2) and 5-LOX (5-lipoxygenase) enzymes. Among all the metal-organic coordination complexes, Zn-PDA (R-6) shows most prominent inhibitory activity than other systems with the IC50 value of 0.0524 μg/mL and 0.834 μg/mL for both COX-2 and 5-LOX enzymes, respectively. The synthesized systems were also evaluated for their activity against COX-1 and standard COX-2 inhibitors viz. Rofecoxib and Aspirin. The rationale for R-6 being the most potent metal complex for dual COX-2 and 5-LOX inhibition is demonstrated using docking studies.
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Citations

Darsi Rambabu, Sharma, S., Mayank, Singh, N., Shagun, & Pooja. (2024). Zn‐Phenanthroline‐Dicarboxylate Complex: A Dual Inhibitor of COX‐2 and 5‐LOX Enzymes. ChemistrySelect, 9(23), e202400310. https://doi.org/10.1002/slct.202400310 (Original work published 2024)