Target-specific rhenium(I) tricarbonyl complexes as prospective pharmacological agents: Synthesis, X-ray crystallography, and in vitro anticancer evaluation

Le résumé fourni par la source

• Four new rhenium(I) tricarbonyl complexes with coordinated picolinic acid and pyrazole ligands were synthesized in high purity and yield. • fac -[Re(5-Br-3-F-Pico)(CO) 3( 3,5-dimethyl-4H-pyrazole)] exhibits promising biological properties against CasKi and MDA-MB-231. • Good correlation in the crystal structures of the synthesized complexes. 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) 3 L2 ] ( 2 ), fac -[Re(5-Br-3-F-Pico)(CO) 3 L1 ] ( 3 ) and fac -[Re(5-Br-3-F-Pico)(CO) 3 L3 ] ( 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 ( 1 H and 13 C), 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 (EC 50 ). The EC 50 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 EC 50 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).

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