Mini Reviews in Medicinal Chemistry - Volume 7, Issue 3, 2007

Several classes of compounds (thioureas, ureas, β-glucosides, sulfonamides, and cyclic peptides) show enhanced binding affinity and selectivity at somatostatin subtype 4 receptors (sst4). Pharmacophore models have recently been proposed to explain receptor subtype selectivity. The chemistry and therapeutic potential of sst4 ligands will be the subject of this review.

Novel compounds have been developed that (in many cases) inhibit cholinesterases and concomitantly interact with at least one further pharmacological target, such as 5-HT3 or H3 receptors. But also enzymes like monoamine oxidase and the serotonin transporter have been targeted. Hybrid molecules can also incorporate antioxidant or neuronal Ca2+- channel-blocking structures.

Increasing number of new drugs, drug formulations and drug delivery systems is evaluated using noninvasive imaging methods. A successful use of new drugs and radiopharmaceuticals depends on their proven quality. This review provides a brief outline of the quality control procedures required for radiolabeled drugs within the context of the existing regulations.

Breast cancer remains a leading cause of death despite early screening and advances in medicine. Bone marrow metastasis often complicates the clinical picture by requiring more aggressive treatment and worsening long-term prognoses. Recent therapeutic targeting of hormonal receptors such as human epidermal growth factor receptor 2 and estrogen receptor has shown limited success in treating localized disease for th Read More

CD26 is a 110 kDa surface glycoprotein with intrinsic dipeptidyl peptidase IV (DPPIV) activity that is expressed on numerous cell types and has a multitude of biological functions. An important aspect of CD26 biology is its peptidase activity and its functional and physical association with molecules with key roles in various cellular pathways and biological programs. CD26 role in immune regulation has been extensively cha Read More

Ethnomedicinal plants have been used as source of candidate drugs for almost all diseases, but the number of compounds having antiviral activity is scarce. Irrespective of type of viruses and the cells they infect, there are a very few specific viral targets for the natural molecules to interact. Most of the available antiviral drugs often lead to the development of viral resistance coupled with the problem of side effects, recurren Read More

Boron Neutron Capture Therapy (BNCT) is a binary cancer treatment that exploits the short range particles released from a nuclear fission reaction involving the non-radioactive 10B nucleus and low-energy (thermal) neutrons for the destruction of tumour cells. If boronated agents are targeted towards chromosomal DNA, the efficiency of BNCT is greatly enhanced. This article presents a concise review of DNA-binding compound Read More

α-tocopherol is a very well-known potent antioxidant and radical scavenger in chemical and biological systems. Its structure has served as starting point for design and synthesis of more potent antioxidant analogues with regard to its potential clinical and nutritional applications in human health. Furthermore, in recent years, intense research has been made not only in the development of hybrid compounds with classical drug moi Read More

Raxofelast, also named IRFI 016 or (±)5-(Acetyloxy)-2,3-dihydro-4,6,7-trimethyl-2-benzofuranacetic acid, belongs to a family of novel molecules designed with the aim to maximize antioxidant potency of phenols related to Vitamin E ( α-tocopherol). This review will focus on the antioxidant and radical scavenging activity of this new promising compound.