Applications of calixarenes in cancer chemotherapy: facts and perspectives

Figures & data

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	^Citation15
	Functionalized with four platinum (II) centers	Anticancer	Growth inhibitory	^Citation17
	Glycoconjugation	Anticancer	Reduction in tumor growth	^Citation18
	Phosphonic, aminophosphonic, and methylenebisphosphonic acid residues	Anticancer	Inhibit phosphatases such as alkaline phosphatase and tyrosine phosphatase	^Citation19
	Hydroxymethylphosphonic acids	Anticancer	Inhibit glutathione S-transferase and prevent multidrug resistance of cancer cells	^Citation20
	Thymine/adenine 2′-deoxynucleotide moieties	Anticancer, antibacterial	Inhibition of DNA replication	^Citation21
	p-sulfonated	Anticancer	Prevent interaction of platelet-derived growth factor and its receptor to prevent angiogenesis	^Citation22,Citation23
	Tetra-amines, methyl and diguanidino groups on the lower rim with tert-butyl, isopentyl, isobutyl and propyl on the upper rim	Anticancer	Angiogenesis inhibitors	^Citation24
	Four Tn antigen glycomimetic units (S-Tn) and an immunoadjuvant moiety (tripalmitoyl-S-glycerylcysteinylserine)	Anticancer	Immune system stimulator against cancer	^Citation29
	Dinuclear platinum compounds	Anticancer	Inhibit tumor growth	^Citation32
	Polyethylene glycol	Anticancer	PDT	^Citation46
Calix[6]arene	Polycationic modification	Anticancer	Inhibits growth	^Citation25
	Imidazole moiety	Anticancer	Upregulates tumor suppressor gene, p53 gene	^Citation26
	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	^Citation27
	p-sulfonated	Anticancer	Photodynamic therapy	^Citation51
Calix[8]arene	Glycoxylation	Anticancer	Prevent tumor migration and proliferation	^Citation30
	TLR2 ligands	Anticancer	Stimulate B lymphocytes for antibody production	^Citation31
	p-sulfonated	Anticancer	PDT via initiation of the apoptotic caspase system, and destruction of the membrane and mitochondria	^Citation51

Abbreviations: PDT, photodynamic therapy; TLR2, Toll-like receptor-2; PI3K, phosphatidylinositide 3-kinase; mTOR, mammalian target of rapamycin.

Figure 1 Cup-shaped representation of calixarene macrocyle with calix[4]arene as an example.

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