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To Preliminarily Evaluate The Anticancer Activiy of 1,2-di(quinazolin-4- yl)diselane Against MDA-MB-435 Cells in vitro

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Breast cancer is the most common invasive cancer among women and a main cause of human death. Chemotherapy drugs play a key role in breast cancer treatment. The current main problems in chemotherapy are drug toxicity and drug resistance. The discovery of antitumor drugs suitable for breast cancer therapy remains one of principal challenges. In our recent anticancer drug discovery screen, 1,2-di(quinazolin-4-yl)diselane (LG003) was found to possess wide spectrum anticancer efficacy. In the present work, the in vitro anticancer activity of LG003 was evaluated in metastatic breast cancer cell line MDA-MB-435. Compared with commercial anticancer drug Gefitinib, Oxaliplatin, Epirubicin Hydrochloride, 10-Hydroxycamptothecin and Taxol, LG003 exhibited better or similar antitumor activity which suggests that LG003 may be a potential anticancer agent for breast cancer. Further treatment time and dose tests indicated LG003 inhibited MDA-MB-435 cells in time- and dose-dependent way. Direct morphological observation showed that LG003 treatment resulted in the decrease in cell population size, then apoptosis like shrinking and blebbing, cell membrane damage and crumbling in turn in a time- and dose-dependent manner. Lactate Dehydrogenase release assay revealed that LG003 executed such effect in MDA-MB-435 cells partly through cytotoxicity which suggests that title compound LG003 can be used as lead compound for the design and synthesis of more active and low toxicity anticancer drugs for breast cancer treatment.
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Keywords: 1; 2-di(quinazolin-4-yl)diselane; MDA-MB-435; anticancer activity; anticancer agent; breast cancer; cytotoxicity

Document Type: Research Article

Publication date: November 1, 2014

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.
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