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Home Biotechnologies Calixarenes For Drug Design

Calixarenes For Drug Design


Disposal of pharmacophoric groups on the molecular platform of calixarenes is profitable direction of biologically active compounds design. Calix[4]arenes substituted with different pharmacophoric groups have shown multifarious biological activity.

The biochemistry of calixarenes has shown rapid development during the past ten years, the highly diverse biomedical applications of these molecules now include antiviral, anti-thrombotic activities, enzyme blocking and protein complexation. The future is even more promising as calixarenes have, now been shown to have potential in the diagnosis of prion-based diseases. Their innocuous nature, as far as is known at present, may open up their future use in medications (Chem. Commun., 2006, 2425–2438).

In the result of the joint project of the Institute of Organic Chemistry NASU, the Institute of Bioorganic and Petrolchemistry NASU and the Institute of Biochemistry NASU it has been demonstrated that calixarenes prove to be versatile molecular platforms for the construction of efficient alkaline phosphatase inhibitors as well as regulators of Ca2+ exchange in the smooth muscle .

The preorganization of phosphonic acid fragments on the calix[4]arene platform results in a significant increase in the inhibition of alkaline phosphatase. The strength of the enzymeinhibitor interactions is determined both by cooperative effects and the goodness of the fit of the inhibitor to the enzyme binding site. Calixarene functionalized at the wide rim with two or four N-sulfonylamidine groups influences Ca2+ transport in Mg2+, ATP-dependent calcium pumps. In this case Ca2+ transport was decreased by 75%. Calixarene-phosphonic acids in concentration 100mM inhibit enzymatic activity of Na+, K+ - ATPase by 86 - 98% and don’t practically affect activity of Mg2+, ATPase. These calixarenes are more efficient than ouabaine in suppressing enzymatic activity of the sodium pump.

Innovative Aspect and Main Advantages

Calixarenes are promising scaffolds for design of phosphatase inhibitors – the medicine-relevant molecules. Inhibition of nonspecific alkaline phosphatases is of significant current medical interest since these enzymes catalyze the hydrolysis of phosphate monoesters, which are involved in a number of important biochemical pathways. The calixarene-methylene-bis-phosphonic acid is one of the most efficient substance among the phosphatase inhibitors described in the literature. The effect of calixarenes on the Ca2+ exchange might be useful for identification of the role of the Mg2+,ATP-dependent Ca2+ pumps of the sarcoplasmic reticulum and plasma membrane in regulation of free Ca2+ concentration in cells.

Areas of Application

Calixarenes are promising materials for nanomedicine application (drug delivery systems, diagnostics, scaffolds for drug design).

Calixarenes For Drug Design
Fig. 1

Stage of Development

A series of calixarene based phosphatase inhibitors and Ca2+ exchange regulators were synthesized in the Institute of Organic Chemistry NASU (see ). The high phosphatase inhibition activity and Ca2+ exchange regulation properties of the calixarenes were examined in the Institute of Bioorganic & Petrolchemistry NASU and in the Institute of Biochemistry NASU (Org. Lett., Vol. 8, No. 4, 2006, p.549-552; Tetrahedron Letters 46 (2005) 7459–7462).

Contact Details

Institute of Organic Chemistry National Academy of Sciences of Ukraine
Murmanskaya str. 5, 02094, Kiev-94, Ukraine
Tel 38 044 551 0616
Fax 38 044 573 2643
E-mail: This e-mail address is being protected from spambots. You need JavaScript enabled to view it

Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine
Murmanska str. 1, 02094, Kyiv-94, Ukraine
Tel 38 044 558 5388

Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine
Leontovicha, 9, 02030 Kyiv-30, Ukraine
Tel. 38 044 234 1653
E-mail: This e-mail address is being protected from spambots. You need JavaScript enabled to view it

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