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A strategy to develop chemotherapeutic agents by combining several active groups into a single molecule as a conjugate that can modulate multiple cellular pathways may produce compounds having higher efficacy compared to that of single-target drugs. In this article, we describe the synthesis and evaluation of an array of dual-acting ER and histone(More)
A series of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives variously substituted at positions 2 and 3 were synthesized and evaluated for their in vitro antiproliferative activities against a panel of six human cancer cell lines. Biological evaluation revealed that the vast majority of derivatives exhibited moderate tumor growth inhibitory activities. In(More)
Five new conjugates of oleanolic acid derivatives and chalcones have been designed and synthesized. The structure elucidation of these conjugates was accomplished by using extensive 1D ((1)H, (13)C) and 2D NMR spectroscopic studies (COSY, HSQC and HMBC); and α-glucosidase inhibitory activity is reported for these conjugates. Compound 2b (IC(50)  = 47.5 µm)(More)
The importance of the heterocyclic core elements with peripheral phenolic and alkyl substituents as a dominant structural motif of ligands for the estrogen receptor (ER) has been well recognized. In this study we expanded the structural diversity of core elements by preparing selenium-containing heterocycles and exploring the activities of these(More)
Five new caged polyprenylated xanthones (1a, 2a, 3, 10a and 10b), and 12 known related compounds were isolated from the resin of Garcinia hanburyi. Their structures were elucidated by detailed spectroscopic analyses and their α-glucosidase inhibitory activities were investigated in vitro. Most of xanthones showed modest inhibitory activity against(More)
Two unique carbazole-indole-type dimeric alkaloids, glycosmisines A (1) and B (2), have been isolated from the stems of Glycosmis pentaphylla and their structures are elucidated by 1D and 2D NMR analyses, and their cytotoxicity against the growth of three cancer cell lines (A549, HepG-2 and Huh-7 cells) in culture was investigated using an MTT assay.(More)
Breast cancer is the most frequent cancer in women worldwide, and incidence is increasing year by year. Although current selective estrogen receptor modulators (SERMs) have clear advantages in the treatment of hormone-responsive breast cancer, they are ineffective for ER(-). In this study, we describe the design and synthesis of a series of dual-acting(More)
A strategy by integrating biological imaging into early stages of the drug discovery process can improve our understanding of drug activity during preclinical and clinical study. In this article, we designed and synthesized coumarin-based nonsteroidal type fluorescence ligands for drug-target binding imaging. Among these synthesized compounds, 3e, 3f and 3h(More)
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