Calixaren α-hydroxymethylenebisphosphonic acids

Title

Calixaren α-hydroxymethylenebisphosphonic acids

Objectives

α-Hydroxymethylenebisphosphonic acids (HMBP) are an important class of drugs used clinically in the treatment of bone diseases involving excessive bone destruction or resorption such as Paget’s disease, osteoporosis and bone metastases. They (who? bones?) are structural analogues of natural pyrophosphates containing a P–C–P backbone and so are stable to enzymatic hydrolysis. More recently, bisphosphonates have been used for treatment of metastatic cancer. It has been shown that these compounds were able to inhibit bone metastases (merge and shorten) proliferation in prostate or breast cancer. They also inhibit experimental angiogenesis in vitro and in vivo. More chemistry, not medicine, please!

Research goals

· the development to develop of methods for the synthesis of calixarenes functionalized on the upper rim of macrocycle by one or two fragments of α-hydroxymethylenebisphosphonic acids;

· the to study of the structure, stereochemistry and association processes of the compounds obtained by methods (NMR does not give us compounds) of NMR, mass-spectroscopy polarimetry, X-ray analysis and molecular modeling;

· the assessment of biological activity of the compounds obtained as inhibitors of alkaline phosphatases.

Expective results

A new type of calixarenes functionalized on at the upper rim by one or two fragments will be synthesized, and investigated for the biological activity, and their physical, and chemical characteristics. Give more chemistry

Graphical abstract Too much - make simpler

Дата добавления: 2015-11-05