Table 1.
Biomedical applications of calixarenes
| Type | Modification(s) | Activity | Mechanism of action | Reference |
|---|---|---|---|---|
| Calix[4]arene | Methylenebisphosphonic and hydroxymethylenebis phosphonic acid groups | Antiobesity, antidiabetic | Inhibitory quality on protein tyrosine phosphatase 1B | 15 |
| Functionalized with four platinum (II) centers | Anticancer | Growth inhibitory | 17 | |
| Glycoconjugation | Anticancer | Reduction in tumor growth | 18 | |
| Phosphonic, aminophosphonic, and methylenebisphosphonic acid residues | Anticancer | Inhibit phosphatases such as alkaline phosphatase and tyrosine phosphatase | 19 | |
| Hydroxymethylphosphonic acids | Anticancer | Inhibit glutathione S-transferase and prevent multidrug resistance of cancer cells | 20 | |
| Thymine/adenine 2′-deoxynucleotide moieties | Anticancer, antibacterial | Inhibition of DNA replication | 21 | |
| p-sulfonated | Anticancer | Prevent interaction of platelet-derived growth factor and its receptor to prevent angiogenesis | 22,23 | |
| Tetra-amines, methyl and diguanidino groups on the lower rim with tert-butyl, isopentyl, isobutyl and propyl on the upper rim | Anticancer | Angiogenesis inhibitors | 24 | |
| Four Tn antigen glycomimetic units (S-Tn) and an immunoadjuvant moiety (tripalmitoyl-S-glycerylcysteinylserine) | Anticancer | Immune system stimulator against cancer | 29 | |
| Dinuclear platinum compounds | Anticancer | Inhibit tumor growth | 32 | |
| Polyethylene glycol | Anticancer | PDT | 46 | |
| Calix[6]arene | Polycationic modification | Anticancer | Inhibits growth | 25 |
| Imidazole moiety | Anticancer | Upregulates tumor suppressor gene, p53 gene | 26 | |
| No modification | Anticancer | Stop signal transduction to AXL and Mer tyrosine kinase receptors overexpressed in pancreatic cancer; it also inhibited the pathway of PI3K/mTOR | 27 | |
| p-sulfonated | Anticancer | Photodynamic therapy | 51 | |
| Calix[8]arene | Glycoxylation | Anticancer | Prevent tumor migration and proliferation | 30 |
| TLR2 ligands | Anticancer | Stimulate B lymphocytes for antibody production | 31 | |
| p-sulfonated | Anticancer | PDT via initiation of the apoptotic caspase system, and destruction of the membrane and mitochondria | 51 |
Abbreviations: PDT, photodynamic therapy; TLR2, Toll-like receptor-2; PI3K, phosphatidylinositide 3-kinase; mTOR, mammalian target of rapamycin.