Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 12, Issue 3, 2012

Apart from review articles, research articles are now also published in Anti-Cancer Agents in Medicinal Chemistry (ACA-MC). This special Editorial Board Issue gathers articles written by ACA-MC Editorial Board Members on the latest developments in various topics and contains both research and review articles. In the first paper, V. Murray and N. Kandasamy report their studies on the sequence specificity of the anti-tumour dr Read More

The sequence specificity of the anti-tumour drug, cisplatin, was determined in a DNA sequence that contained seven telomeric repeats and a run of ten consecutive guanine bases. Cisplatin preferentially forms DNA adducts at consecutive guanine sequences. Hence these DNA sequences were examined in order to gain an insight into the important human genomic regions that are damaged by cisplatin. A polymerase stop/linear Read More

Molecules that inhibit histone deacetylases (HDACs) activity have shown a great promise as anticancer agents since they interfere with cell proliferation and angiogenesis, induce cell differentiation and promote apoptosis. A number of HDACIs (for example: SAHA) have been approved by FDA for the treatment of cancer in different stages of clinical trials. HDAC inhibition proves to be a worthy strategy for cancer therapy. T Read More

Advanced cancers of the prostate and breast commonly progress by metastasizing to the skeleton, where they are incurable but cause serious morbidity and contribute to mortality. Growth of tumor in bone takes several years, opening a large window for pharmaceutical prevention of metastatic progression. Bone provides a unique microenvironment for tumor growth, including niches occupied by hematopoietic and m Read More

Protein kinases are important enzymes in solid tumour and leukaemia pathologies. Their structures are well understood at the atomic level and their key role in the progression of certain cancers makes them valuable targets for anti-cancer therapy. Through medicinal chemical approaches, we developed an efficient preparative stereospecific synthesis of N12, N13 pyran-bridged indolocarbazoles that opens access to functio Read More

Melanoma is the most aggressive form of skin cancer and advanced stages are inevitably resistant to conventional therapeutic agents. In particular, epigenetic strategies might open interesting new perspectives in combination with conventional ones. Current therapeutic strategies, in particular for metastatic melanoma, do not give great results in terms of survival. Herein, I review HDACis and microRNAs for melanom Read More

Curcumin, one of the most studied chemopreventive agents, is a natural compound extracted from Curcuma longa L. Extensive research over the last half century has revealed that curcumin can inhibit the proliferation of various tumor cells in culture, prevent carcinogen induced cancers in rodents and inhibit the growth of human tumors in xenotransplant or orthotransplant animal models. Several phase I and phase II clinica Read More

The Vinca alkaloids are a group of widely used anticancer drugs, originally extracted from the Madagascar periwinkle, that disrupt microtubule dynamics in mammalian cells by interfering with proper assembly of α,β-tubulin heterodimers. They favor curved tubulin assemblies that destabilize microtubules and induce formation of spiral aggregates. Their binding energy profiles have been characterized by means of Read More

Cell death plays an important role in cancer growth and progression, as well as in the efficiency of chemotherapy. Although apoptosis is commonly regarded as the principal mechanism of programmed cell death, it has been increasingly reported that several anticancer agents do not only induce apoptosis but other forms of cell death such as necrosis, autophagy and mitotic catastrophe, as well as the state of permanent lo Read More

In the last decades, NGR-containing peptides have been proved useful for ligand-directed targeted delivery of various chemotherapeutic drugs to tumor vasculature. Aminopeptidase N (APN; CD13) has been demonstrated to be a key binding site for NGR peptides on tumor vasculature. For drug targeting, chemical means have been applied to couple NGR-peptides to small molecule drugs, such as cytokines, antiangiogenic c Read More

Histone deacetylases (HDACs) are a family of conserved metalloproteases which play a key role in the development of cancer. They can be divided into 18 subtypes according to their structural diversity. Histone deacetylase inhibitors are considered as potential anti-cancer agents and a lot of pan-HDAC inhibitors have entered clinical trials. Selective HDAC inhibitors targeting only one member or one class subtype are less expl Read More

Genistein, one of the predominant isoflavones derived from soybeans, has been shown beneficial effects in cancer prevention and treatment. There is an accumulating body of experimental evidences suggesting that genistein affects cancer progression by increasing apoptosis, inducing cell cycle arrest,modulating intracellular signaling pathways, and inhibiting invasion and metastasis of cancer cells. During last decade, Read More