Concomitant chemoradiotherapy for inoperable non-small cell carcinoma of the lung: results of continuous infusion Cisplatin in 85 patients

Reboul, F.; Vincent, P; Chauvet, B.; Brewer, Y.; C, Fauré; Taulelle, M.

doi:10.1007/978-2-8178-0765-2_77

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“…Non‐small cell lung cancer (NSCLC) is the most deadly form of this disease and has a 5 year survival rate below 15% . Platinum‐containing chemotherapies, DNA intercalators such as doxorubicin and etoposide and protein kinase inhibitors such as lapatinib and imatinib can be used to treat NSCLC. This range of treatment options is necessary to reduce patient specific side‐effectsand to avoid disease resistance in certain subpopulations .…”

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confidence: 99%

Design, synthesis, and evaluation of the anticancer activity of 2‐amino‐aryl‐7‐aryl‐benzoxazole compounds

et al. 2017

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A series of 2-amino-aryl-7-aryl-benzoxazole derivatives have been designed, synthesized, and evaluated as anticancer agents. Fourteen of the compounds exhibited cytotoxic effects toward human A549 lung cancer cells. We found 12l was the most potent with an EC of 0.4 μm, equivalent to the anticancer drug doxorubicin, but had low selectivity following cross screening in monkey kidney Vero cells. Eight of the most potent or most selective compounds were further profiled in additional cell lines (MCF7, NCI-H187, and KB) to better understand their cytotoxic activity. Only compound 12l had a measurable EC in a single cell line (3.3 μm in the KB cell line). Taken together, this data suggest the series as a whole display specific cytotoxicity toward A549 cells. Cheminformatics searches pointed to JAK2 as a possible target. A subset of compounds assayed at this target showed IC s ranging from 10 to 0.08 μm; however, no clear correlation between JAK2 potency and A549 cytotoxicity was observed.

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