Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 17, Issue 2, 2017

Breast cancer is the most common cancer and the most frequent cause of cancer death among women worldwide. Breast cancer is a complex, heterogeneous disease classified into hormone-receptor-positive, human epidermal growth factor receptor-2 overexpressing (HER2+) and triple-negative breast cancer (TNBC) based on histological features. Endocrine therapy, the mainstay of treatment for hormone-responsive br Read More

It is a longstanding debate whether cancer is one disease or a set of very diverse diseases. The goal of this paper is to suggest strongly that most of (if not all) the hallmarks of cancer could be the consequence of the Warburg‘s effect. As a result of the metabolic impairment of the oxidative phosphorylation, there is a decrease in ATP concentration. To compensate the reduced energy yield, there is massive glucose uptake, an Read More

Photodynamic therapy (PDT) is an alternative cancer treatment to conventional surgery, radiotherapy and chemotherapy. It is based on activating a drug with light that triggers the generation of cytotoxic species that promote tumour cell killing. At present, PDT is mainly used in the treatment of wet age-related macular degeneration, for precancerous conditions of the skin (e.g. actinic keratosis) and in the palliative care of adv Read More

Epigenetic modifications can affect numerous mechanisms used by neoplastic cells to evade immune control. In melanoma epigenetic defects, caused by dysregulations in the expression of genome writers, erasers, or readers, play a significant role in the reduced expression of molecules required for efficient immune recognition as well as antigen presentation and processing. Alterations in gene expression were identified Read More

Background: Due to the high level of argininosuccinate synthase (ASS), a key enzyme for the formation of arginine from citrulline, human breast cancers are often resistant to arginine deprivation therapy. An antimetabolite, Lcanavanine (L-CAV), can be incorporated into proteins in the place of arginine, disturbing protein conformation and leading to cellular death. Objectives: This study was designed to investigate the potenti Read More

Background: The RAPTA-EA1 complex [ruthenium(II)-arene 1,3,5-triaza-7-phosphaadamantane (pta) complex with an arene-tethered ethacrynic acid ligand] has been reported to overcome drug resistance that developed due to the current use of platinum-based treatments. However, the exact mechanism of action of RAPTA-EA1 remains largely unexplored and unknown. Objective: Here we have further studied the effect Read More

Background: Lectins are carbohydrate-binding proteins that exhibit remarkable antitumor activities by inducing apoptotic or autophagic cell death. However, the relationship between apoptosis and autophagy induced by lectins has rarely been reported. Agrocybe aegerita lectin (AAL), a lectin isolated from the fungus Agrocybe aegerita, exerts antitumor activity through apoptosis. Objective: To study the relationship between th Read More

Background: Microtubules act as a useful and strategic molecular target for various anticancer drugs that binds to its distinct sites in tubulin subunits and inhibits its polymerization and ultimately leads to cell death. Moreover, numerous reports highlight the cytotoxic effects of constraint Combretastatin analogs and thiazolidinone derivatives. Objective: Therefore, the present study investigates the potential of thiazolidinon Read More

A total of 16 targeted NO-releasing betulinic acid (BA) derivatives were designed and synthesized as potential anticancer agents. Most IC50 values were under 1.0 μM in vitro test against HepG2 and B16. The result suggested that derivatives of BA with α,β-unsaturated ketone skeleton possessed significant cytotoxic activities than the others, among which derivatives with three carbons in diol linker (15b and 15c) exhibited the high Read More

Enzymatic activity from tumor and adjacent normal tissue of 200 patients involving deoxycytidine kinase (dCK), uridine/cytidine kinase (U/CK), cytidine deaminase (CD) and deoxycytidylate deaminase (dCMPD) was quantified. Patients with brain (17), colon (24), and breast (30) tumors, 53, 67, and 73%, respectively, had an elevated T/N value (Specific Activity of tumor/ Specific Activity of normal tissue) involving dCK and dC Read More

Background: Bruton’s Tyrosine Kinase (BTK) is a one of the Tec tyrosine kinase family. It has an essential role in B-cell development and function. Activation of BTK has been associated with the pathogenesis of many types of lymphomas and leukemia, and involved in non-life threatening autoimmune diseases. Objective: In this study, exhaustive pharmacophore modeling was combined with QSAR analyses to examine the Read More

Background: Coumarins are naturally occurring plant metabolites and several synthetic coumarin analogues are known for their various pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties. Objective; Keeping this promising pharmacological properties in mind, in the present investigation, mono/dihalogenated coumarin analogues CMRN Read More

Background: Hepatocellular carcinoma (HCC) is related to chronic liver inflammation. M2 polarization of tumor-associated macrophages (TAMs) in the tumor microenvironment promotes liver cancer stem-like cell (LCSLC) self-renewal capability and carcinogenicity. Therefore, reversing M2 polarization of TAMs could be an effective approach to cure HCC. Objective: To evaluate whether 8-bromo-7-methoxychrysin (BrMC) has Read More

Background: A novel formulation for cabazitaxel loaded HSA nanoparticle (Cbz-NPs) with non-crosslinking agent participation was reported in this study. Objective: A simple method through unfolding of HSA self-assembling nanoparticle for cabazitaxel (Cbz) overcomes the drawbacks of Cbz with high toxicity, poor solubility and low tissue specificity, and avoids side effects of polysorbate 80 which is commonly used for dissolvi Read More

Background: Topical chemotherapy of skin cancers is a promising strategy for reduction of side effects and for improvement of patient compliance. The combination of the chemotherapeutic 5-fluouracil (5-FU) and the anti- EGFR antibody cetuximab is a strategy to inhibit tumor growth. Their skin penetration, however, is hampered by their high hydrophilicity, which could be improved by encapsulation in delivery systems. Furtherm Read More