Synthesis, characterization and urease inhibition, in vitro anticancer and antileishmanial studies of Co(III) complexes with N,N,N′-trisubstituted acylthioureas

Abstract

The series of cobalt(III) complexes (1a–12a) with N,N,N′-trisubstituted acylthioureas were synthesized and characterized by FT-IR, and multinuclear (1H and 13C) NMR spectroscopy and LC–MS combined with elemental analysis. Crystal structure of cobalt(III) chelate of type Co(L-O, S)3 were determined by single crystal X-ray diffraction analysis. Complexes were adopted to have the octahedral geometry, where the fac-disposed N,N,N′-trisubstituted acylthioureas showed bidentate mode of coordination environment at cobalt centre defined by three O and three S donor atoms. The ligands are coordinated in a chelate fashion, forming three five-membered rings. The synthesized complexes were screened against Jack bean urease. In vitro anticancer activity against lung carcinoma (H-157), and kidney fibroblast (BHK-21) cell lines of the synthesized compounds were also studied and found them potent candidates for drugs. Cytotoxic results revealed that compound 10a was emerged as a leading member with an IC50 value of 0.75±0.027μM against H-157 cell lines. When synthesized compounds were tested for antileishmanial activity against the promastigote forms of Leishmania major, compound 4a was identified as the most potent and lead candidate showed highest inhibition with an IC50 value of 0.45±0.053μM.