期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 24, 期 19, 页码 4731-4740出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.08.016
关键词
PARP-1/2; Inhibitors; Tricyclic; Anticancer
资金
- National Natural Science Foundation of China [81502928]
- Outstanding Scientific and Technological Innovation Team of Jiangsu Province of China
- Fundamental Research Funds for the Central Universities [2015PY015]
8,9-Dihydro-2,4,7,9a-tetraazabenzo[cd]azulen-6(7H)-ones were designed and synthesized as a new class of PARP-1/2 inhibitors. The compounds displayed a variable pattern of PARP-1/2 enzymes inhibition profile that, in part, paralleled the antiproliferative activity in cell lines. Among them, compound 9e exhibited not only the significant IC50 value of 28 nM in the PARP-1 and 7.7 nM in PARP-2 enzyme assay, but also a profound synergic efficacy combined with temozolomide with PF50 values of 2.6, 2.5, and 6.5 against MDA-MB-468, SW-620 and A549 and cell line, respectively. (C) 2016 Elsevier Ltd. All rights reserved.
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