- Total synthesis of dysidavarone A
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Dysidavarone A is a sesquiterpene isolated from the South China Sea sponge Dysidea avara and was reported that it showed significant anticancer activities. Because the compound has unique ‘dysidavarane’ carbon skeleton and potent biological activity, a se
- Yu, Chunhui,Zhang, Xiaoguang,Zhang, Jinghua,Shen, Zhengwu
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- In vitro study and structure-activity relationship analysis of stilbenoid derivatives as powerful vasorelaxants: Discovery of new lead compound
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The development of vasorelaxant as the antihypertensive drug is important as it produces a rapid and direct relaxation effect on the blood vessel muscles. Resveratrol (RV), as the most widely studied stilbenoid and the lead compound, inducing the excellent vasorelaxation effect through the multiple signalling pathways. In this study, the in vitro vascular response of the synthesized trans-stilbenoid derivatives, SB 1-8e were primarily evaluated by employing the phenylephrine (PE)-precontracted endothelium-intact isolated aortic rings. Herein we report trans-3,4,4′-trihydroxystilbene (SB 8b) exhibited surprisingly more than 2-fold improvement to the maximal relaxation (Rmax) of RV. This article also highlights the characterization of the aromatic protons in terms of their unique splitting patterns in 1H NMR.
- Chan, Sock Ying,Loh, Yean Chun,Oo, Chuan Wei,Yam, Mun Fei
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- Synthesis and potent antileukemic activities of 10-benzyl-9(10H)-acridinones
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A novel series of 10-benzyl-9(10H)-acridinones and 1-benzyl-4-piperidones were synthesized and tested for their in vitro antitumor activities against CCRF-CEM cells. Assay-based antiproliferative activity study using CCRF-CEM cell lines revealed that the acridone group and the substitution pattern on the benzene unit had significant effect on cytotoxicity of this series of compounds, among which 10-(3,5-dimethoxy)benzyl-9(10H)-acridinone (3b) was found to be the most active compound with IC50 at about 0.7 μM. Compound 3b was also found to have antiproliferative activity against two other human leukemic cell lines K562 and HL60 using the MTT assay. The antitumor effect of 3b is believed to be due to the induction of apoptosis, which is further confirmed by PI (Propidium iodide) staining and Annexin V-FITC/PI staining assay using flow cytometry analysis.
- Gao, Chunmei,Jiang, Yuyang,Tan, Chunyan,Zu, Xuyu,Liu, Huachen,Cao, Derong
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p. 8670 - 8675
(2008/12/23)
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- Discovery and structure-activity studies of a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors
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The inhibition of tyrosine kinase-mediated signal transduction pathways represents a therapeutic approach to the intervention of proliferative diseases such as cancer, atherosclerosis, and restenosis. A novel series of pyrido[2,3-d]pyrimidine inhibitors of the PDGFr, bFGFr, and c-Src tyrosine kinases was developed from compound library screening and lead optimization.' In addition, highly selective inhibitors of the FGFr tyrosine kinase were also discovered and developed from this novel series of pyrido[2,3-d]pyrimidines. The syntheses, biological evaluation, and structure-activity relationships of this series are reported.
- Connolly, Cleo J. C.,Hamby, James M.,Schroeder, Mel C.,Barvian, Mark,Lu, Gina H.,Panek, Robert L.,Amar, Aneesa,Shen, Cindy,Kraker, Alan J.,Fry, David W.,Klohs, Wayne D.,Doherty, Annette M.
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p. 2415 - 2420
(2007/10/03)
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