Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 15, Issue 9, 2015

Phenanthroindolizidine and phenanthroquinolizidine derivatives constitute a series of compounds that are being intensively studied as potential anticancer agents. Related natural products such as antofine and tylophorine alkaloids are well known for their high cytotoxic activity; however, their clinical application has been limited because of their side effects. In this review we report, in detail, on the main structural modifica Read More

Cancer is known to be the second most common disease-related cause of death among humans. In drug discovery programs anti-cancer chemotherapy remains quite challenging due to issues related to resistance. Plants used in traditional medicine are known to contribute significantly within a large proportion of the African population. A survey of the literature has led to the identification of ~400 compound Read More

Flavonoids, a diverse class of polyphenolic compounds, are well known for their anticancer properties. Moreover, it is generally accepted that these plant secondary metabolites can also sensitize malignant cells to conventional chemotherapeutic drugs and could thus be considered as potential adjunctive agents in cancer treatment. In this review article we show that besides potentiating the anticancer activity of standard chem Read More

Protein neddylation, a newly characterized posttranslational modification that adds the ubiquitin-like molecule NEDD8 to substrates, modulates important biological processes, whereas dysfunction of neddylation may cause several serious diseases, such as cancer. Inhibition of neddylation pathway has emerged as a promising anticancer strategy, as evidenced by development of the NEDD8-activating enzyme (NAE) inhibito Read More

Onset of tumors in breast cancer is a multi-factorial event at different ages and ethnic populations. The conventional treatment strategy suggests use of anti-estrogen drugs and selective estrogen receptor modulators (SERMs). Although, this strategy has achieved significant success to prevent tumor growth and metastasis and is still developing under an active field of research, the emergence of immunotherapy is a potential m Read More

Background: Ovarian cancer (OC) is the most lethal of gynecologic tumors because women generally present with advanced stage disease. Platinum-based chemotherapy play a pivotal role in OC treatment. The aim of the study was to assess the effects of CAP-regimen chemotherapy on blood redox status in patients with ovarian cancer. Materials and Methods: Patients were 132 women with primary OC with FIGO stage III Read More

21 new structures of isoxazole-moiety-containing thieno[2,3-d]pyrimidine derivatives(3a~3u) were synthesized for the first time and characterized using IR, 1H NMR, 13C NMR, ESI-MS and elemental analysis techniques. And then their in vitro anticancer activity against lung cancer A549, colorectal HCT116 and breast cancer MCF-7 cell lines was preliminarily evaluated using the MTT method. Among them, most compound Read More

Multidrug resistance (MDR) refers to cross-resistance to a range of structurally and functionally unrelated compounds, and is accompanied by an elevated expression of ATP driven cell-membrane transporters. The cytotoxicity of Malabaricone-A (MAL-A), a diarylnonanoid derived from Myristica malabarica was demonstrated in leukemic cell lines, but its effectiveness in drug-resistant cancer cell lines has not been evalua Read More

Maleimides consist of an important class of compounds easily synthesized with multiple functional group modification that provides expressive pharmacological properties including, antitumoral activity, mediated mainly by oxidative stress. For this reason, the present study was designed to evaluate the cytotoxicity and the role of reactive oxygen species (ROS) in maleimide-induced cell death. Cell viability assays were perfor Read More

Benzimidazole ring is a versatile structure which has been extensively utilized in medicinal chemistry. Since we are working on 1,2-disubstutited benzimidazoles, we have reported new antitumor active derivatives. As a continuation to our previous work, we have synthesized a new series of 1-(2-aryl-2-oxoethyl)-2-[(N,Ndimethylamino/ pyrrolidinyl/piperidinyl)thiocarbamoyl] benzimidazole derivatives. Anticancer activity of the co Read More

Our previous study indicated that nontoxic doses of quercetin (Que) could increase the chemosensitivity of breast cancer cells to doxorubicin (Dox) although the mechanism still remains elusive. Therefore, in this study, we aimed to investigate the underlying mechanisms. MCF-7 cells and MCF-7/dox cells were exposed to PTEN inhibitor bpV (HOpic), Dox, or combination of Dox and Que with or without bpV (HOpic) intervention fo Read More

C6 rat glioma cells are one of the most aggressive carcinogenic tumors, due to its high mortality rate in human beings and animals. The current treatment for this illness includes surgery, radio and chemotherapy, showing relapse in patients treated with those therapies. Since the ozone was found to be an effective bioreactive to inhibit growth of several carcinoma cells in vitro and in vivo. In this research, therapeutic peritone Read More

Genistein is a bioactive isoflavone derived from soybeans. The tie-in between the intake of genistein and the decreased incidence of some solid tumors (including prostate cancer) has been demonstrated by epidemiological studies. The potential of genistein in treating prostate cancer has also been displayed by in vitro cell-based and in vivo animal experiments. Genistein has entered clinical trials for both chemoprevention Read More

Cutaneous squamous cell carcinoma (CSCC) is one of the most common cancers worldwide, requiring effective therapeutic interventions. Retinoids are important chemopreventive and therapeutic agents for a variety of human cancers including CSCC. In this study we synthesized a novel retinoic derivative N-(4-ethoxycarbonylphenyl) isoretinamide (ECPIRM) and evaluated its biological activities and possible mechanisms in human Read More