Two series of podophyllotoxin derivatives were synthesized by addition a 4?-sulfanilamide to or substitution 4?-amide into podophyllotoxin. Their cytotoxicities evaluated against four human cancer cell lines (A549, HeLa, MCF-7, and PC-3). Investigations the structure–activity relationship generalized. Derivative 9f (2-thienoylaminoepipodophyllotoxin) exhibited highest activity cells, inhibiting...

PURPOSE Chemotherapies for breast cancer generally have strong cellular cytotoxicity and severe side effects. Thus, significant emphasis has been placed on combinations of naturally occurring chemopreventive agents. Silibinin is a major bioactive flavonolignan extracted from milk thistle with chemopreventive activity in various organs including the skin, prostate, and breast. However, the mecha...

Background: Molecular targeted therapy by different cell death inducers are recently considered in cancer therapy. The aim of this study was to compare the effect of cisplatin and inositol trisphosphate kinase inhibitor (caffeine) on human breast cancer cell line (MCF-7). The pattern of cell death in MCF-7 cells following the exposure to cisplatin and caffeine in individual and combination form...

PURPOSE The aim of these studies was to characterize the action of STX140 in a P-glycoprotein-overexpressing tumor cell line both in vitro and in vivo. In addition, its efficacy was determined against xenografts derived from patients who failed docetaxel therapy. EXPERIMENTAL DESIGN The effects of STX140, Taxol, and 2-methoxyestradiol (2-MeOE2) on cell proliferation, cell cycle, and apoptosis...

Herein we describe the synthesis of five new 2-aryl and 2-alkylimidazolone derivatives via an effective one-pot synthetic strategy assisted by microwave irradiations which allowed us to access desired product in a reduced time reaction compared thermal heating slightly better yield (48% 45%). The imidazolone were evaluated for their anticancer activity vitro against MCF-7, MDA-MB-231 HepG2 cell...

Models of long-term estrogen-deprived breast cancer cells are utilized in the laboratory to mimic clinical aromatase inhibitor-resistant breast cancer and serve as a tool to discover new therapeutic strategies. The MCF-7:5C and MCF-7:2A subclones were generated through long-term estrogen deprivation of estrogen receptor (ER)-positive MCF-7 cells, and represent anti-hormone‑resistant breast canc...

Objective (s): In chemotherapy for cancer treatment, the cell resistance to multiple anticancer drugs is the major clinical problem. In the present study, mesoporous silica nanoparticles (MSNs) were used as a carrier for epirubicin (EPI) in order to improve the cytotoxic efficacy of this drug against the P-glycoprotein (P-gp) overexpressing cell line. Materials and Methods: MSNs with phosphonat...

Objective: To investigate the antioxidant and cytotoxic activities of sulfur-containing glycine imine derivatives MCF-7 (human breast adenocarcinoma) DLD-1 (colorectal cell lines. Methods: This study examined (25-200 µM) via DPPH, metal chelating reduction methods. Furthermore activity MCF-7, MCF-12A (normal epithelial) DLD-1, CCD-18CO colon fibroblast) were with MTT (3-(4,5-Dimethylthiazol-2-y...

In this work, we used microwave irradiation conditions to synthesize β-enaminonitrile (4), which was affirmed using single crystal X-ray diffraction and the different spectral data. Two tumor cell lines, MCF-7 MCF-7/ADR, as well two normal HFL-1 WI-38, were assess anticancer activity of compound 4. The studied molecule exhibited potent efficacy against MCF-7/ADR lines compared with reference dr...

Protein kinase C (PKC) modulates growth, differentiation and apoptosis in a cell-specific fashion. Overexpression of PKC-alpha in MCF-7 breast cancer cells (MCF-7-PKC-alpha cell) leads to expression of a more transformed phenotype. The response of MCF-7 and MCF-7-PKC-alpha cells to phorbol esters (TPA) was examined. TPA-treated MCF-7 cells demonstrated a modest cytostatic response associated wi...