Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 17, Issue 3, 2017

Radionuclide antibody conjugates (RACs) and antibody-drug conjugates (ADCs) can function as biotherapeutic missiles in order to target cancer cells and destroy them. The advent of new technology platforms consisting of imaging modalities, drug design and radiochemistry will facilitate the personalised approach for cancer patient treatment programmes. The utilisation of radionuclides and cytotoxic drugs conjugated to bio Read More

Since its first description in 1955, tumor hypoxia has become a central issue in cancer treatment. Since then, it is essential to diagnose accurately the tumor oxygenation degree in order to establish the appropriate treatment. In this regard, a wide diversity of radiopharmaceuticals for in vivo imaging has been developed. Special conditions of the hypoxic microenvironment are low O2 partial pressure, enhanced levels of reduc Read More

Cancer remains as one of the major causes of death worldwide. The emergence of nanotechnology has opened new avenues for the development of nanoparticle (NP)- based diagnostic and therapeutic tools. NPs of different chemical composition, size, shape and surface decoration can be prepared using a wide variety of synthetic strategies. Subsequent radiolabelling with positron or gamma emitters results in potential dia Read More

Background: The use of nanobiomaterials is increasing each day. Among the immense variety of nanomaterials developed and studied the hydroxyapatite is one of the most ones. Objective: In this study we developed and tested nano-hydroxyapatite dopped with Ho-166 for bone cancer. Results: The results showed that the nano-hydroxyapatite dopped with Ho-166 has a great affinity for the bone. Conclusion: The pre-clini Read More

Background: Chemotherapy is one of the most common approaches for cancer treatment. Particularly Doxorubicin has been proven to be effective in the treatment of many soft and solid tumors for locally advanced and metastatic cancer. It is not easy to clinically evaluate the chemotoxic or chemoprotective effect of some drugs, even more when there is a subclinical toxicity. Objective: To determine the usefulness of the hep Read More

Pancreatic cancer is one of the most aggressive human cancers and is expected to surpass breast cancer to become the third chief cause of cancer-related deaths in the United States. While conventional treatment approaches such as surgery and classic chemotherapy have slightly improved the relative five year survival rate to 8% yet it is the lowest survival rate for any major cancer. This emphasizes the serious ne Read More

Breast cancer is the heterogeneous disease and leading cause of death in women, worldwide. It is generally caused by the perturbation of various signaling pathways responsible for cell apoptosis. Due to genetic variability, different signaling pathways are disrupted in different breast cancer patients; so, to overcome this multifaceted condition, the personalized treatment is preferred. Since, various potential targets exist in br Read More

Metabolic reprograming contributes to esophageal tumorigenesis. A better understanding of how esophageal cancer (EC) cells reactivate primitive signaling to retain glucose metabolism under unfavorable conditions is essential for the development of therapeutic interventions to treat EC. Current achievements in the field of EC glucose metabolism have been critically reviewed to address several fundamental questions. Th Read More

Background: Coumarins possess a broad spectrum of biological activities and are important pharmacophores in drug developments. Since aberrant upregulation of PI3K/Akt signaling is related to uncontrolled tumor cell proliferation, enhanced migration, and adhesion-independent tumor growth, it is of interests to find novel coumarin derivatives as anticancer agents targeting the PI3K/Akt signaling pathway. Objective: A variety of Read More

Background: The number of cancer cases around the world has increased according to the World Health Organization (WHO) reports, nearly 14 million new cases and 8.2 million cancer associated mortalities have been reported in 2012. Chemotherapeutic resistance is a major problematic issue in the management of patients with breast tumor. Objective: In this study, the apoptotic gene profile of 4T1 mouse breast cancer c Read More

Background: Inflammation substantially contributes to the development and progression of malignancies. cancer-related inflammation, has been proposed to promote tumor progression and serve as the seventh hallmark of tumor. Tumor microenvironment, products of inflammatory cells influence almost every aspect of tumorigenesis and tumor progression. Objective: The aim of this study was to design and evaluate dru Read More

Background: Copper has shown to be useful in disorders with an inflammation origin such as cancer [1-3]. It has previously shown that Casiopeínas® interact with DNA and promote the disruption by a mechanism related to the increase in the level of free radicals [4-6] which confers antineoplastic potential. Objetive: The aim of the present work was to study the antitumor effects of a series of Cu(II) complexes with sa Read More

Background: Poly(hydroxyalkanoates) (PHA) have recently attracted increasing attention due to their biodegradability and high biocompatibility, which makes them suitable for the development of new prolong drug formulations. Objective: This study was conducted to develop new prolong paclitaxel (PTX) formulation based on poly(3- hydroxybutyrate) (PHB) microparticles. Method: PHB microparticles loaded with antitumor Read More

Background and Objective: The clinical success of the chemotherapeutic drugs is restricted by the nonspecific toxicity-related adverse side effects. The diverse implication of indoles and thiazoles in medicinal chemistry prompted us to develop a new series of novel 2-aryl-amino-4-(3′-indolyl)thiazoles as more effective and less toxic anti-cancer compounds. Method and Results: One-pot microwave-assisted rapid and hig Read More

Background: The present study emphasizes on designing a new series of isatin-dihydropyrimidinone derivatives by adopting a hybrid pharmacophore approach. Fe3O4 nanoparticles (Fe3O4 NP) are magnetically recoverable and are effective catalysts adequately used to synthesize Isatin-dihydropyrimidinones. Individual derivatives of Isatin and dihydropyrimidinone are equipotent to treat cytotoxicity. Objective: The Read More

Background: Globally, cancer is regarded as one of the biggest health concern in humans and animals and is one of the most terrifying diseases. Therefore, there is a necessity for the discovery, development and improvement of novel antitumor drug molecules which could efficiently prevent proliferative pathways and clonal expansion of cells. Heterocyclic compounds like benzochromene play a key role in the development of Read More