Medicinal chemistry. Natural products inspired molecular design

The search for new therapeutic agents is a great scientific challenge for synthetic organic chemists. The "Biology Oriented Synthesis" (BIOS) and the "Function Oriented Synthesis" (FOS) postulate the design of novel molecules inspired by natural products using simple "chemical structures" that provide new molecular functions. Privileged structures derived from natural products have evolved over millions of years optimizing specific interactions with proteins, enzymes, and other biological systems. In particular, we focus on the application of efficient methodologies using few reaction steps, purifications by crystallization and one-pot or multicomponent reactions generating the least amount of waste possible in the design of new derivatives of chalcone-type polyphenolic compounds as well as other flavonoids. Likewise, it is a scientific and social challenge to use those molecules, efficiently isolated from natural sources, as starting products to generate new bioactive compounds.

In this research line, we examined the effects of either natural and synthetic compounds inspired in natural products on the growth of several human cancer cell lines (leukemia, acute myeloid leukemia HL-60, chronic myeloid leukemia K-562, human histiocytic lymphoma U-937, lymphoblastic leukemia MOLT-3, human B cell precursor leukemia NALM-6) and cell lines over-expressing Bcl-2 (U-937/Bcl-2) and the glycoprotein P (K-562/ADR).