Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 14, Issue 6, 2014

After water, tea is the most widely consumed beverage. The major active constituents in green tea are catechins, of which epigallocatechin-3-gallate (EGCG) is the most abundant and active compound. Animal experimental studies using EGCG alone or green tea catechins with EGCG being a major component have generated a mounting body of evidence suggesting that EGCG as a naturally occurring compound and commo Read More

Cancer stem cells are a subset of cells that are responsible for cancer initiation and relapse. They are generally resistant to the current anticancer agents. Successful anticancer therapy must consist of approaches that can target not only the differentiated cancer cells, but also cancer stem cells. Emerging evidence suggested that the dietary agent curcumin exerted its anti-cancer activities via targeting cancer stem cells of v Read More

Garlic (Allium sativam L.) is widely used in traditional herbal remedies and alternative medicine. The potential health benefits of garlic are largely attributed to its metabolic byproducts. Extensive in vivo and in vitro studies has demonstrated that the garlic derivatives possess anti-cancer effects, but the underlying mechanisms are not completely understood. In this mini-review, we aim to summarize the reported biological Read More

Prostate cancer is common in men with very high mortality which is one of leading causes of cancer-related deaths in men. The main treatment approaches for metastasized prostate cancer are androgen deprivation and chemotherapeutic agents. Although there are initial responses to castration, the resistance to the treatment will eventually occur, leading to castration-resistant prostate cancer. The common chemothe Read More

Resveratrol (3, 5, 4’-trihydroxy-trans-stilbene, RVT), a stilbenoid, polyphenol phytochemical present in berries, grape, peanuts and wine. It has been suggested as a major contributor to “French Paradox” that reduces the mortality from coronary heart disease (CHD) by consuming RVT in red wine even in some of French population with a high-fat intake. With extensive research, it has been found that RVT is a versatile and pleiotrop Read More

Quercetin, a natural protective bioflavonoid, possesses diverse pharmacologic effects, such as antioxidant, anti-inflammatory, anti-proliferative, and anti-angiogenic activities. Recently, quercetin’s effect in cancer prevention and treatment was recognized. However, the poor water solubility and low-bioavailability of quercetin limit its clinical use in cancer therapy. Nanotechnology provides a method to create novel formulatio Read More

Paris polyphylla J.E. Smith is extensively used in traditional systems of Indian and Chinese medicines mainly for its anticancerous property. The national and international demand for P. polyphylla is constantly increasing and most of the supplies come from wild. Illegal and unscientific exploitation coupled with habitat destruction decreases the natural population of the herb, as a consequence this species comes under v Read More

Rho GTPases play a key role in the regulation of multiple essential cellular processes, including actin dynamics, gene transcription and cell cycle progression. Aberrant activation of Rac1, a member of Rho family of small GTPases, is associated with tumorigenesis, cancer progression, invasion and metastasis. Particularly, Rac1 is overexpressed and hyperactivated in highly aggressive breast cancer. Thus, Rac1 appears to be a p Read More

Objectives: To study the effect of co-injecting unlabelled hypericin (Hyp) on biodistribution, necrosis uptake and tumour retention of iodine-123 or iodine-131 labelled hypericin (123/131I-Hyp), a necrosis avid agent for an anticancer radiotherapy. Methods: 123/131I-Hyp was prepared with Iodogen as oxidant and formulated in 0.6 μg/kg no-carrier-added (NCA) or 0.25 mg/kg unlabelled Hyp carrier-added (CA) forms using di Read More

The present work describes the anticancer activity of a new indolylcoumarin named COUFIN and more specifically, its efficiency against clear cell renal carcinoma (CCRC). COUFIN inhibited microtubule formation and bound on tubulin to or near the colchicine site. In vitro, COUFIN showed potent anticancer activity on renal carcinoma cells (RCC) both in monolayer (2D culture) (IC50 of 88±8 nM) and multicellular tumor sphe Read More

Recent era aims at developing safer partial Peroxisome proliferator-activated receptor-γ (PPAR- γ) agonists in order to dodge the toxicity issues related to full agonists. With a view to develop non-thiazolidinediones as partial PPAR-γ agonists, novel analogues of oxazol-5-ones (3a-3q) were designed and virtually analyzed for their molecular and drug like properties. The newly synthesized compounds were further evaluated f Read More

Numerous studies showed that drug resistance of gastric cancer cells could be modulated by the abnormal expression of microRNAs (miRNAs) which target multiple cell signaling pathways. The possible function of miR-1271 in the formation of cisplatin resistance in gastric cancer cells has been investigated in this study. miR-1271 was significantly down-regulated in gastric cancer tissues and various gastric cancer cell lines. Read More

We developed a drug-delivery system comprising a novel platinum drug (Pt(II) complex) entrapped within β-Casein (β-CN) nanoparticles referred to as nano-vehicles. Fluorescence spectroscopy, UV-Vis spectrometry, dynamic light scattering (DLS), and scanning electron microscopy (SEM) were used to characterize the β-CN-Pt(II) complex . What was apparent in this study was that the solubility of Pt (II) complex increased in the Read More

Objectives: Honey is reported to contain various compounds such as antioxidants. Chrysin is a natural and biologically active compound extracted from honey. It possesses antioxidant properties and promotes cell death by perturbing cell cycle progression. We focused on the possible role that chrysin may act as a potential anticancer agent, and tested its biological activity and possible mechanisms in the human lung adenocarc Read More

Synthesis of new chiral thiourea derivatives (27 examples) as anticancer agents has been described. Three compound 7d (NSC code 761448/1), 7e1 (NSC code 767161/1), and 7e3 (NSC code 767160/1) were found to exhibit higher anticancer activity than 5-fluorouracil against Colon cancer, Melanoma, Ovarian cancer, and Breast cancer subpanels. The effect of stereochemistry of amino acid residues on the tumor growth inh Read More