Heterocyclic architecture for the synthesis of anti-HIV protease and anti-cancer compounds

Introduction of heterocycle moieties in a bioactive molecule can have important effects on physicochemical and pharmacological properties, because of their chemical stability, their structural rigidity and due to the improving bioavailability and aqueous solubility1. Therefore the possibility of H-bond interaction with target backbone atoms can increase their efficacy. The success of this strategy in identifying new biologically active molecules in distinct therapeutic areas has gained a significant growth and different heterocycle are introduced in biological molecules2. In particular organic scaffold containing heterocycles have been described as “privileged structures” since they are capable of binding to many receptors with high affinity3. Of particular interest is the fact that most know chemicals are based on heteroarene frameworks4,5. There are a range of fused [5,6] ring systems that exhibit biological activity. In particular fused [5,6] ring systems, used in the synthetic paths discussed in this work, include indole, benzofuran and benzothiophene. From several years, in the laboratory where I did my PhD work, research is focused on the introduction of heterocyclic structures into molecules with potential inhibitory activity against the HIV virus. The study concerned the synthesis of compounds designed to block the action of the HIV protease (HIV-Pr), an essential enzyme for the production of mature HIV particles. .. [edited by Author]