Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 12, Issue 7, 2012

Matrix metalloproteinases (MMPs) are known to participate in cancer invasion and metastasis. Copious research on MMPs and their inhibitors has promoted the understanding of the mechanisms of cancer invasion and metastasis as well as the development of effective drugs for cancer treatment. This review discusses the classification of MMPs and tissue inhibitors of metalloproteinases (TIMPs) in relation to tumor growt Read More

Five decades of extensive research have passed since the description for the first time of the existence of an enzyme, which had the ability to degrade collagen during the metamorphosis of tadpoles. In fact, during these years, a large family of enzymes possessing the unique ability of degrading the extra cellular matrix (ECM) has been discovered. These enzymes are widely known as Matrix Metalloproteinases (MMPs) a Read More

Reversion-inducing-cysteine-rich protein with Kazal motifs (RECK) is a membrane-anchored glycoprotein that negatively regulates the activities of matrix metalloproteinases (MMPs) and inhibits tumor invasion, metastasis, and angiogenesis. RECK is essential for normal development and is a key mediator of tissue remodeling and stabilization of tissue architechture. Downregulation of RECK documented in a wide range of maligna Read More

MMPs are a family of Zn dependent endopeptidases, which can mediate degradation of ECM components during various physiological and pathological processes including cancer. Some ECM components, through interaction with integrin receptor and modulation of downstream signaling, are capable of regulating expression and activity of several MMPs. α5β1 integrin is the universally accepted receptor for the E Read More

MicroRNAs have come to represent a significant mechanism of post transcriptional gene regulation affecting processes as varied as cellular differentiation, proliferation, metabolism, apoptosis, and cancer. As more miRNAs are unravelled and their roles dissected, it has become evident that the involvement of these molecules in cancer is much more extensive than initially thought. Several miRNA expression analyses in b Read More

Lung cancer is a heterogeneous disease with several histologic subtypes. The two major pathologies, which account for approximately 70% of lung cancers, are adenocarcinoma (AD) and squamous cell carcinoma (SQ). Traditionally, these two subtypes have been categorized as non-small-cell lung cancer and treated similarly. However, they are different not only pathologically, but also functionally. For example, 18F-fluorodeox Read More

Hepatocellular carcinoma (HCC) is a cancer with extremely poor prognosis. This review discusses the pathological characteristics of multi-step hepatocarcinogenesis, tumor growth, invasion and metastasis, the expression of matrix metalloproteinases (MMPs) and their inhibitors via signal transduction in relation to dedifferentiation of hepatoma cells. It introduces the reports on anti-cancer agents in the field of MMP science Read More

In the United States, about 22,000 women will be diagnosed with ovarian cancer in 2011, and an estimated 14,000 patients will succumb to the disease [1]. Surgery and chemotherapy present the main treatment modalities, but despite the development of novel therapies, the overall 5 years survival for ovarian cancer patients with advanced disease at diagnosis remains at only about 30%. Novel therapeutic strategies are nee Read More

Melanoma is the most severe skin cancer characterized by a bad prognosis at metastatic stages due to resistance to most classical chemotherapies. Invasion of melanoma cells into the surrounding microenvironment locally and at distance of the primary tumour, is facilitated by expression of proteases that degrade the extracellular matrix. Matrix metalloproteinases (MMP) have been long thought as potential the Read More

Emetine and CGP-74514A have previously shown antitumor activity in neuroendocrine tumor cell lines. The aim of this study was to investigate the cytotoxic activity of the drugs in a three-dimensional model and to study if the mechanism of the cytotoxic activity was induction of apoptosis. An in vitro hollow fiber model was used to study the cytotoxic effect and a multiparametric high-content screening assay was used for measur Read More

Malignant cells in solid tumors survive under prolonged hypoxia and can be a source of resistance to current cancer therapies. Tumor hypoxia is also associated with a more malignant phenotype and poor survival in cancer patients. Recent progress in our understanding of the biology of tumor cells under hypoxia has led to increased attention on targeting hypoxia for cancer therapy. We report here that a novel fusicoccin Read More

A series of N-substituted amino caproic hydroxamic acid histone deacetylase inhibitors derivatives was designed in good-toexcellent yields and evaluated for their antiproliferative activity in a panel of human cancer cell lines, showing half maximum effective concentration varying from 700 nM to > 100 μM. Interestingly, the replacement of a furyl group by a thienyl one impacted very significantly the cap role on this antiproli Read More

The analysis of the influence of molecular features which can be extracted from the simplified molecular input line entry system (SMILES) and involved in the process of the building up of a series of QSAR models (with different splits into training and test sets) by means of the CORAL software for mutagenicity and anticancer activity has been performed. The presence of nitrogen (sp3) is favorable for decrease of the b Read More

All chemotherapeutic agents currently in use have a narrow window of therapeutic index of 1 to 1.2. Camptothecin ester compounds are reported to have a wider therapeutic index when being used to treat human xenografts in nude mice. As a continuous effort in searching for better chemotherapeutic agents for treating cancers, new haloalkyl camptothecin and 9-nitrocamptothecin ester derivatives 2a-b and 3a-d we Read More

R (rituximab)-CHOP (cyclophosphamide, adriamycin, vincristin, and prednisone) is given to outpatients with CD20-positive lymphoma as a standard treatment. However, this regimen requires long-term infusion because of the necessity for monitoring the infusion reaction (IR) during R administration. In this study, pharmacological changes in anti-tumor agents were examined after the joint use of R and CHOP, and the p Read More