BN80927 belongs to a novel family of camptothecin analogs, the homocamptothecins, developed on the concept of topoisomerase I (Topo I) inhibition and characterized by a stable seven-membered -hydroxylactone ring. Preclinical data reported here show that BN80927 retains Topo I poisoning activity in cell-free assay (DNA relaxation) as well as in living cells, in which in vivo complexes of topoiso...

Figitumumab (CP-751,871), a potent and fully human monoclonal anti-insulin-like growth factor 1 receptor (IGF1R) antibody, has been investigated in clinical trials of several solid tumors. To identify biomarkers of sensitivity and resistance to figitumumab, its in vitro antiproliferative activity was analyzed in a panel of 93 cancer cell lines by combining in vitro screens with extensive molecu...

Despite the potential of type 1 interferons (IFNs) for the treatment of cancer, clinical experience with IFN protein therapy of solid tumors has been disappointing. IFN-beta has potent antiproliferative activity against most human tumor cells in vitro in addition to its known immunomodulatory activities. The antiproliferative effect, however, relies on IFN-beta concentrations that cannot be ach...

Lignosus rhinocerus, the tiger milk mushroom, is one of the most important medicinal mushrooms used by the indigenous people of Southeast Asia and China. It has been used to treat breast cancer. A cold water extract (LR-CW) prepared from the sclerotia of L. rhinocerus cultivar was found to exhibit antiproliferative activity against human breast carcinoma (MCF-7) and human lung carcinoma (A549),...

The expression of the forkhead transcription factor checkpoint suppressor 1 (CHES1), also known as FOXN3, is reduced in many types of cancers. We show here that CHES1 decreases protein synthesis and cell proliferation in tumor cell lines but not in normal fibroblasts. Conversely, short hairpin RNA-mediated depletion of CHES1 increases tumor cell proliferation. Growth suppression depends on the ...

CONTEXT Medullary thyroid carcinoma (MTC) is a rare tumor originating from thyroid parafollicular C cells. It has been previously demonstrated that insulin-like growth factor I (IGF-I) protects MTC from the effects of antiproliferative drugs. Everolimus, an mTOR inhibitor, has shown potent antiproliferative effects in a human MTC cell line, TT, and in two human MTC primary cultures. OBJECTIVE...

objective(s) as an important class of natural products, coumarins exhibit many biological activities and the diversity of their bioactivity is so huge that the pharmacological promiscuity has been applied on their case. oxypeucedanine also named as prangolarin is a linear furanocoumarin with an oxygenated prenylated substitution at c-5 of the nucleus. to our knowledge, there are few reports on ...

Fluorinated 2-(4-amino-3-methylphenyl)benzothiazoles possess potent antiproliferative activity against certain cancer cells, similar to the unfluorinated 2-(4-amino-3-methylphenyl)benzothiazole (DF 203, NSC 674495). In "sensitive" cancer cells, DF 203 is metabolized by, can induce expression of, and binds covalently to CYP1A1. Metabolism appears to be essential for its antiproliferative activit...

Purpose: To evaluate the influence of a humic-fulvic acid substance on quantitative yield residual foci DNA double-strand break (DSB) repair protein-marker - phosphorylated histone H2AX (γH2AX) and proliferation activity in culture human mesenchymal stromal cells (MSCs) 24, 48, 72 h after exposure to X-ray radiation at doses 2, 4 10 Gy. Material methods: Through 24 hours incubation MSCs with ac...

In this study, we investigated the growth inhibitory effects of IFN-α, 5-FU, HU and their combinations on Daudi (Human Burkitt lymphoma) and K562 (Human erythroblastic leukemia) cell lines. Sensitivity of two leukemia cell lines to IFN-α has shown large disparities. While Daudi cells were very sensitive to the antiproliferative effects of IFN-α, K562 cells were more resistant. After showing dif...