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- Title
Synthesis, characterization and urease inhibition, in vitro anticancer and antileishmanial studies of Ni(II) complexes with N, N, N′-trisubstituted thioureas.
- Authors
Rauf, Muhammad; Yaseen, Samad; Badshah, Amin; Zaib, Sumera; Arshad, Raffia; Imtiaz-ud-Din; Tahir, Muhammad; Iqbal, Jamshed
- Abstract
A series of N, N, N′-trisubstituted thioureas ( 1-12) and their Ni(II) complexes ( 1a-12a) were synthesized and characterized by multinuclear (H and C) NMR, FT-IR spectroscopy and LC-MS techniques in combination with elemental analysis. The crystal structures of both ligands and Ni(II) chelates of type Ni(L- O, S) were determined by single crystal X-ray diffraction analysis. All the complexes were adopted to have square planar geometry, where the N, N, N′-trisubstituted thioureas showed bidentate mode of coordination at nickel centre through oxygen and sulfur atoms. The synthesized complexes were screened for potential inhibitors of Jack bean urease. Compounds 1a and 3a were observed as most potent inhibitors of urease exhibiting IC values of 1.17 ± 0.12 and 1.19 ± 0.41 µM, respectively. Cytotoxicity assay on lung carcinoma (H-157) and kidney fibroblast (BHK-21) cell showed that compounds were significant anticancer agents. Additionally, the complexes were tested against Leishmania major and found to be potent antileishmanial agents.
- Subjects
UREASE; IN vitro studies; ANTINEOPLASTIC agents; NICKEL; SUBSTITUTION reactions; THIOUREA
- Publication
Journal of Biological Inorganic Chemistry (JBIC), 2015, Vol 20, Issue 3, p541
- ISSN
0949-8257
- Publication type
Article
- DOI
10.1007/s00775-015-1239-5