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Inflammation is often an exacerbating factor in breast cancer and elicits tumor tissue infiltrating and metastases,and the Tamoxifen resistance is also one of the most serious problems for breast cancer therapy.In this presentation,we will report series of novel small molecules with dual regulation activity,which including novel selective estrogen receptor modulators(SERMs) with both anti-proliferative and anti-inflammatory activities;novel selective estrogen receptor downregulators (SERDs) for Tamoxifen resistance cancer cell;novel organometallic SERMs with anti-proliferative activity for both ER positive(ER+) and ER negative(ER)resistance breast cancer cell.