Target-specific rhenium(I) tricarbonyl complexes as prospective pharmacological agents: Synthesis, X-ray crystallography, and in vitro anticancer evaluation.
Ramoba, Lesetja V. Macharia, Lucy W. Chakraborty, Suparna Prince, Sharon Malan, Frederick P. Alexander, Orbett T. Manicum, Amanda-Lee E.
Ramoba, Lesetja V.
Macharia, Lucy W.
Chakraborty, Suparna
Prince, Sharon
Malan, Frederick P.
Alexander, Orbett T.
Manicum, Amanda-Lee E.
Citations
Altmetric:
Abstract
Rhenium tricarbonyl complexes have been investigated primarily due to their remarkable inhibitory effects against cancerous cells. This study presents the synthesis, solid-state crystallography, and in vitro biological evaluation of four rhenium(I) tricarbonyl complexes. The synthesized complexes: fac-[Re(Pico)(CO)3(L1)] (1), fac-[Re(Pico)(CO)3L2] (2), fac-[Re(5-Br-3-F-Pico)(CO)3L1] (3) and fac-[Re(5-Br-3-F-Pico)(CO)3L3] (4); where L1 = 3,5-dimethyl-1H-pyrazole, L2 = 3 (trifluoromethyl)-5-methyl-1H-pyrazole, and L3 = 3,5-diphenyl-1H-pyrazole; were characterized with FT-IR, NMR (1H and 13C), UV-Vis spectroscopy, and single-crystal X-ray diffraction technique. Preliminary in vitro biological screening of these complexes at a concentration of 10 μM in DMSO (solvent) indicated that only complex 3 exhibited significant cell viability against HeLa (61.38 ± 9.55), CaSki (52.00 ± 2.78), and MDA-MB-231 (30.50 ± 4.72) cancer cell lines. Consequently, this complex was further evaluated for its half-maximal effective concentration (EC50). The EC50 values for complex 3 were determined to be 45.6 ± 0.09 μM (selectivity index [SI] = 0.31), 19.87 ± 0.21 μM (SI = 0.71), and 6.0 ± 0.15 μM (SI = 2.36) against HeLa, CaSki, and MDA-MB-231 cells, respectively, with an EC50 value of 14.15 ± 0.23 μM against MRC-5 (normal human cells). Moreover, apoptosis and Western blot analyses reveal that complex 3 successfully induces apoptosis in cervical cancer cell lines (HeLa and CaSki) as well as in the triple-negative breast cancer cell line (MDA-MB-231).
Description
Date
2025-09-15
Journal Title
Journal ISSN
Volume Title
Publisher
Elsevier
Collections
Research Projects
Organizational Units
Journal Issue
Keywords
Rhenium(I) tricarbonyl, Systhesis, X-ray crystallography, In vitro cytotoxicity