Cancer is one of the leading causes of death in the world. Therefore new improved chemotherapeutic agents are needed. The tambjamines are a class of marine alkaloids with intriguing pharmacological properties, including antitumor activity. Inspired in the structure of these compounds we have synthesized a family of synthetic analogs displaing interesting antitumor activity "in vitro", promoting apoptosis in several cancer cell lines.
New and innovative aspects
The compounds described in this invention display interesting antitumor activity "in vitro" showing low toxicity against normal cells. Their action mechanism is proposed to be their ionophoric activity. These compounds can function as anion carriers upsetting the ionic balance of cells. They are cytotoxic and through thios activity they induce apoptosis indifferent cellular cancell lines.
Main advantages of its use
The mechanism of action of these compounds allow them to be used in resistant cell lines against conventional chemotherapies.
Specifications
The compounds described in this invention are inspired by the structure of marine alkaloid bearing a 4-methoxybipyrrol unit. Substitution of this moiety by different enamine group yields the active derivatives. These compounds can promote the transmembrane transport of anions such as chloride an bicarbonate.The ionophoric activity of these compounds change the intracelular pH of the treated cells. Vital tinction assays using acrinidine orange revealed the deacidification of acidic organelles such as lysosomes. It is known that this process triggers apoptosis and IC50 values in the low micromolar range were calculated for these compounds in different cancer cell lines.
Applications
These compounds should be of interest for pharmaceutilcal companies willing to conduct preclinical studies to assess their potential in the clinic. They can be used for the treatment of different cancer conditions.
Intellectual property status
Protected by patent P201201039
Current development status
Research or Experimental
Desired business relationship
Commercial Agreement, License Agreement, Technical Cooperation: further development; Technical Cooperation: testing new applications; Technical Cooperation: adaptation to specific needs.
The aim of the The Technology Transfer Office (TTO) of the Univesidad de Burgos is to promote Innovation technology through the reseach results transfer and the conexions between the University and the new needs and requirements of the society - we are the link between the University and the Industry. Contact person: José Manuel López (jmllopez@ubu.es)
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