AbstractThis is a review of the literature concerning the interesting properties of p-, d-, and f-block elements when coordinated with 2,6-pyridinedicarboxylic acid (dipicolinic acid, H2 dipic) and its derivatives as ligands, with a focus on their use as inorganic pharmaceuticals. Some of the complexes reported were used as insulin-like, bioimaging contrasting agents, antimicrobial agents, and anticancer agents.
× 10 5 and 1.6 × 10 4 M −1 , respectively). Topoisomerase inhibition assays and cleavage studies proved that complex 4 was an efficient catalytic inhibitor of human topoisomerases I and IIα. Based upon the results obtained from the 3-(4,5-dimethylthiazol-2-yl)-5-(3carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay on 4T1-luc metastatic mammary breast cancer cells (IC 50 = 34.4 ± 5.2 μM when compared to IC 50 = 13.75 ± 1.08 μM for the control, cisplatin), further investigations into the molecular events initiated by exposure to complex 4 were investigated. Studies have shown that complex 4 activated both the apoptotic and autophagic signaling pathways in addition to causing dissipation of the mitochondrial membrane potential (ΔΨ m). Furthermore, activation of cysteine-aspartic proteases3 (caspase 3) in a time-and concentration-dependent manner coupled with the ΔΨ m , studies implicated the intrinsic apoptotic pathway as the major regulator of cell death mechanism.
A series of half-sandwich ruthenium complexes, two containing an arene face-cap and the other a thiacrown ether face-cap were synthesized to investigate the necessity of the arene for anticancer activity in this class of compounds. The complexes are formulated as [(η 6 -p-cymene)Ru(dmabTSC)Cl]PF 6 , [(η 6 -benzene) Ru(dmabTSC)Cl]PF 6 (arene complexes), and [([9]aneS 3 (dmabTSC)Cl]PF 6 (dmabTSC = dimethylaminobenzaldehye thiosemicarbazone). It was observed that none of the complexes showed good anticancer activity in vitro against HCT-116 and Caco-2 (colon adenocarcinoma) cells. All three complexes can bind strongly to calfthymus DNA with binding constants on the order of 10 5 M -1 . In addition they all bind strongly to human serum albumin with binding constants between 10 5 and 10 6 M -1 . There appears to be a single binding site on the protein for these complexes. A computational investigation of these complexes and their hydrolysis products was carried out by molecular docking with DNA and topoisomerase II. From this analysis it is noted that the type of face-capping ligand had different effects on the two macromolecules. It is therefore noted that the knowledge gained from this study will be useful in identifying the type of complexes in this class that show useful metallodrug potential.
PDT is a suitable treatment option for several diseases however there are several challenges and limitations. The incorporation of NPs in the field of PDT is an extremely promising avenue which can be utilized to improve the execution of PDT. Furthermore, the use of inorganic compounds was noted to be frequented in the development of PSs and NP conjugates. The patents presented addressed the associated problems with PDT but there still remains an opportunity for continued research efforts so that more clinical applications are possible.
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