Stereselective Synthesis of Antitumoral and Antiviral Compounds

The research activity of the group focuses on the synthesis of antitumoral and antiviral compounds and on the development of new synthetic strategies to streamline their preparation. It is organized into three main research lines:

Total synthesis of cytotoxic macrolides. The Amphidinolides are a family of marine natural product macrolides with potent cytotoxic activity. Isolation from the organisms that produce them yields very small amounts of these interesting compounds. Total synthesis is indispensable to obtain enough material to fully study their biological activity and mode of action. Analysis of the interactions of these compounds with their target proteins, in silico, can aid in the understanding their bioactivity and in the design of simplified analogues, potentially useful as drugs for the treatment of cancer. We have already completed the total syntheses of several Amphidinolides and studied their binding with actin, a cytoskeletal protein involved in cell division and in cancer cell motility. We are currently working on the total synthesis of Amphidinolides B₁/B₂ and Iriomoteolide 2a.

Microbicides. Currently, there are around 37 million people suffering from HIV infection. Microbicides are the most promising, general, and cheap anti-AIDS agents for preventing HIV-1 transmission, particularly for women in less-developed countries. We are working on the development of novel microbicides by conjugation of standard vaginal gels with known entry inhibitors.

Organocatalysis. Organic compounds have been employed for many years as catalysts but their use only became widespread in the first years of this century, when secondary amines such as proline were used as catalysts in several transformations. We are interested in this field both from a synthetic and mechanistic standpoint and are now studying the intermediates formed in the aminocatalyzed nitro-Michael reaction and the application of the products obtained to total synthesis.