Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 17, Issue 4, 2017

Cancer patients, though frequently entering complete remission after successful surgery, and/or irradiation, and chemotherapy years or even decades later may exhibit overt metastases and aggressive, mostly fatal recurrence on the basis of clinically silent persistence of disseminated tumor cells. Cellular dormancy is a mode of hibernation/ inactivity caused by a temporary mitotic arrest. It represents the critical pheno Read More

Cancer incidence represents an important public health problem worldwide. Nuclear factor kappa B (NF- ΚB) transcription factor plays a pivotal role in the regulation of genes that control various responses in eukaryotic cells, including proliferation and survival, cytoskeletal remodeling, cellular adhesion and apoptosis. Extensive studies have demonstrated the contribution of NF-ΚB transcription in the promotion and progression Read More

Triple negative breast cancer (TNBC) is a heterogeneous disease entity constituting about 15% of breast cancer cases worldwide. TNBC is associated with poor prognosis and lack of sustained response to conventional chemotherapeutic agents. Tumoral heterogeneity and the presence of several subtypes of TNBC such as Basal like (BL)-1, BL-2, immune-modulatory, luminal androgen receptor, mesenchymal, and mesen Read More

The chemistry of heterocyclic containing, 1,3,4-thiadiazole has been an interesting field of study from ancient years. Subsequently, 1,3,4-thiadiazole nucleus constitutes a significant class of compounds for new drug development. Recently, various 1,3,4-thiadiazole derivatives synthesized and evaluated their biological activities including antimicrobial, antituberculosis, antioxidant, anti-inflammatory, anticonvulsants, antidepress Read More

Background: Peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor that regulates the expression of many genes relevant to carcinogenesis. By analogy to selective estrogen receptor modulator for treatment of cancer, selective or partial PPARγ agonists are considered clinically important for chemotherapy of cancer. Objective: In this study we have rationally modified the structure of existing Read More

Background: Cancer is one of the severest diseases in the world, and lung cancer is one of the five common cancers causing thousands of deaths every year. Moreover, most of the lung cancer patients die because of bone metastasis. Methods: This research was conducted with the aim of developing novel nanoparticles (NPs) of docetaxel (DTX) loaded bovine serum albumin (BSA) conjugated docosahexaenoic acid (DHA) us Read More

Background: Microtubules are dynamic filamentous cytoskeletal proteins which have used widely in cancer chemotherapy. Generally, the action of these compounds depends on binding to the tubulin proteins which are α , β-heterodimers that form the core of the microtubules. Arylthioindoles (ATIs) inhibit tubulin polymerization by binding to the colchicine site, inhibiting the binding of colchicine to tubulin. QSAR modeling play a Read More

Background: Betulinic acid is a lupane-type triterpene firstly extracted from the bark of white birch. It has displayed anti-inflammatory, antioxidant, anti-HIV and selective cytotoxicity. Objective: To understand the structure- anti-tumor activity relationship of betulinic acid and betulin derivatives and to synthesize novel anti-tumor derivatives of betulinic acid and betulin. Method: The 3D-QSAR methods including CoMFA and CoMSI Read More

Background: Cancer is one of the most serious clinical problems worldwide, and considerable efforts have been devoted to discovering therapeutic agents with novel modes of action. Natural and synthetic coumarin derivatives have attracted intense research interest due to their diverse structural features and remarkable array of biological properties. Objective: In the present study, we synthesized a series of 4-MU deriv Read More

Background: Cancer is characterized by uncontrolled cell division caused by dysregulation of cell proliferation. Therefore, agents that impair cancer cell proliferation could have potential therapeutic value. Higher plants are considered to be a good source of anticancer agents, and several clinically tested chemotherapeutic agents have been isolated from plants or derived from constituents of plant origin. Methods: In the pr Read More

Background: Curcumin is a natural hydrophobic product showing anticancer activity. Many studies show its potential use in the field of cancer treatment due to its safety and efficiency. However, its application is limited due to its low water-solubility and poor selective delivery to cancer. Objective: A Y-shaped folic acid-modified poly (ethylene glycol)-b-poly (-caprolactone)2 copolymer was prepared to improve curcumin so Read More

Background: Efficacy of multimodality approaches for the treatment of squamous cell cancer of the head and neck has remained unsatisfactory and further advances are critically required. Targeted cell death induction is a novel therapeutic approach that may help to improve clinical management of Head and Neck cancer patients. Objective: The potency of novel hybrid benzoxazole-coumarins on the induction of apo Read More

Background: Fisetin,quercetin and kaempferol are among the important representatives of flavonols, biological active phytocomounds, with low water solubility. Objective: To evaluate the antimicrobial effect, respectively the antiproliferative and pro apoptotic activity on the B164A5 murine melanoma cell line of pure flavonols and their beta cyclodextrins complexes. Method: Incorporation of fisetin, quercetin and kaempferol Read More

Background: Zanthoxylum capense (small knobwood) is a South African species known for a wide range of anecdotal uses. However, there is a dearth of information on its phytoconstitutional make-up, specifically its knobs, with only a few reports on the bioactive compounds that could justify its ethnomedicinal use. Objectives: This work aimed to identify the active principles in Z. capense and evaluate their cytotoxicity a Read More

Background: Some bioactive peptides derived from natural resources or synthesized by rational design have been shown to have very good anticancer effects. We designed an anticancer fusion peptide (ACFP) based on the structure of bovine lactoferricin (LfcinB) and hexapeptide (PGPIPN) derived from bovine milk protein. Objective: To prepare ACFP through genetic engineering and study its antiovarian cancer acti Read More