My research activity has focused on the synthesis of biologically active synthetic or natural compounds. The synthesis of most of them is based on the functionalization of polyhalogenated heteroaryl compound, by reaction with organometallic catalyzed by transition metals. In fact the two publications with more number of citations are related to this synthetic methodology (Tetrahedron, Bioorg. Med. Chem. Lett.). This methodology has allowed us to develop simple synthetic routes allowing to obtain quickly a variety of compounds with important biological activities (Org. Biomol. Chem, ChemBioChem). The objective of this project poses to use this methodology for the synthesis of spirobifluorenes. The synthesized of this compounds have applicability in the field of materials.
The second part of my research career focuses on the synthesis of derivatives with potential anticancer activity. This research is conducted in a European project (Epitron). The synthesis of natural compounds with anticancer activity was performed: Psammaplin A (Thesis Jose Garcia) and Bisaprasin (Thesis Santiago Perez). The synthesis of Psammaplin A (Bioorg. Med. Chem) allowed us to develop a study of structure-activity relationship (SAR). The most important analogs described was UVI5008 (J. Med. Chem., Mol. Cancer Ther.), it is a compound derived from tryptophan and cysteine, which has a very promising anticancer activity. The results of the synthesis of this compound are the items of highest impact. Also we have developed two patents on this derivative.
Gronemeyer, Hinrich; Altucci, Lucia; De Lera, Angel; Stunnenberg, Hendrik Gerard. “Psammaplin A derivatives as HDAC inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer”. WO2008125988(A1), 2008-10-23
Gronemeyer, Hinrich; De Lera, Angel; Altucci, Lucia A method for the synthesis of derivatives of psammaplin A, and their use for the prevention or treatment of cancer EP1964835 (A1), 2008-09-03
The second part of my research career focuses on the synthesis of derivatives with potential anticancer activity. This research is conducted in a European project (Epitron). The synthesis of natural compounds with anticancer activity was performed: Psammaplin A (Thesis Jose Garcia) and Bisaprasin (Thesis Santiago Perez). The synthesis of Psammaplin A (Bioorg. Med. Chem) allowed us to develop a study of structure-activity relationship (SAR). The most important analogs described was UVI5008 (J. Med. Chem., Mol. Cancer Ther.), it is a compound derived from tryptophan and cysteine, which has a very promising anticancer activity. The results of the synthesis of this compound are the items of highest impact. Also we have developed two patents on this derivative.
Gronemeyer, Hinrich; Altucci, Lucia; De Lera, Angel; Stunnenberg, Hendrik Gerard. “Psammaplin A derivatives as HDAC inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer”. WO2008125988(A1), 2008-10-23
Gronemeyer, Hinrich; De Lera, Angel; Altucci, Lucia A method for the synthesis of derivatives of psammaplin A, and their use for the prevention or treatment of cancer EP1964835 (A1), 2008-09-03
