Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity.

A novel series of indolocarbazoles were synthesized and their antiproliferative activity against HUVEC, LoVo, DLD-1 and ST-486 cell lines, was investigated. Those staurosporine analogs in which a substituted dimethylaminoalkoxy chain was attached to the indolic nitrogen showed interesting activity and selectivity with respect to HUVEC proliferation. The effect on capillary tube formation in 3-dimensional matrigel matrix was studied using the most active compounds.

Discovering a new analogue of thalidomide which may be used as a potent modulator of TNF-alpha production.

A new series of imide derivatives related to thalidomide were synthesized and evaluated as modulators of TNF-alpha production. These derivatives enhance TNF-alpha production using human leukemia HL-60 cells induced with 12-O-tetradecanoylphorbol 13-acetate (TPA), while inhibiting TNF-alpha production induced with okadaic acid (OA) in the same cell line. The diphenylmaleimide derivative 2f, was found to be the most active product, producing a strong modulation of the cytokine level.

Reorganization of enynes catalyzed by platinum salts.

Activation of alkynes with platinum salts allows their reaction with alkenes, giving rise to a myriad of interesting processes like cyclizations, formation of cyclopropanes, or metathesis. Weak nucleophiles can also participate in the processes leading to alkoxycyclizations. There are intriguing mechanistic aspects of these processes in which subtle variations of the reaction conditions and/or substrate structures can lead to completely different products.

The Pauson-Khand reaction, a powerful synthetic tool for the synthesis of complex molecules.

There are still some synthetic chemists who hesitate to use metal-mediated or -catalysed reactions. The Pauson-Khand reaction (PKR) is a powerful transformation that has now been sufficiently well developed to be routinely considered when planning a synthesis, especially of polycyclic complex molecules. This tutorial review aims to encourage the use of this process explaining the best ways of performing a PKR both in the stoichiometric and the catalytic version, showing the scope of the process and its limitations.

Synthesis and biological evaluation of novel bisindolylmaleimides that inhibit vascular endothelial cell proliferation.

A novel class of bisindolylmaleimides were synthesized and antiproliferative activities (HUVECs and three tumor cell lines) of these compounds were investigated. Two water-soluble derivatives, 10 and 12, possessing a dimethylaminoalkoxy side chain in their structure, showed interesting activity and selectivity on HUVECs proliferation.