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	1. Design, synthesis and prelimnary biological activity studies of dithiocarbamate-3-epi-Jaspine B hybrids
	Zhang En,Wang,Shang,Jiao,Wei-Wei,Xu,Jin-Mei,Liu,Hong-Min
	Pharmacy 17 April 2015
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	Abstract:A series of dithiocarbamate-3-epi-Jaspine B hybrids were designed and synthesized from D-xylose. Lipophilic long alkyl dithiocarbamate was introduced to C4 position of 3-epi-jaspine B in the new molecules. Their anticancer activity against two selected tumor cell lines (MGC-803 and B16-F10) were evaluated. Most synthesized compounds exhibited moderate activity against MGC-803 and B16-F10. Among them, compound 16d showed best inhibition against MGC-803 (IC50 = 16.39 μM). Compound 16f exhibited best inhibition against B16-F10 (IC50 = 14.83 μM). This is the first report about the synthesis and in vitro cytotoxic evaluation of dithiocarbamate -3-epi-jaspine B hybrids.
	TO cite this article:Zhang En,Wang,Shang,Jiao,Wei-Wei, et al. Design, synthesis and prelimnary biological activity studies of dithiocarbamate-3-epi-Jaspine B hybrids[OL].[17 April 2015] http://en.paper.edu.cn/en_releasepaper/content/4639429


	2. Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa
	DONG Wenfang,GUO Ju,LIU Wei,YAN Zheng,WANG Nan,LIU Zhanzhu
	Pharmacy 08 March 2013
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	Abstract:Fifteen simplified tetrahydroisoquinoline analogues were prepared from L-dopa. The in vitro antitumor activities of these analogues were evaluated against HCT-8, BEL-7402, BGC-823, A549, A2780, MCF-7 and MX-1 cell lines. The IC50 values of the cytotoxicity of most analogues were at the level of 10-7M or 10-8M. Compound 17 with 2,3,4-trimethoxycinnamate side chain at C-22 showed the most potent antitumor activity.
	TO cite this article:DONG Wenfang,GUO Ju,LIU Wei, et al. Synthesis and cytotoxicity of 3-arylacrylic ester derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa[OL].[ 8 March 2013] http://en.paper.edu.cn/en_releasepaper/content/4527983

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	3. A convenient way to synthesize bufadienolactam analogs with inhibitory activity against the prostate cancer cells
	Xiao-Feng Yuan,Hai-Yan Tian,Juan Li,Shu-Tai Jiang,Ken Wing-Keung Liu,David A. Middleton,Wen-Cai Ye,Ren-Wang Jiang
	Pharmacy 28 February 2013
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	Abstract:Bufadienolactam (1) and secobufalinamide (2) were synthesized by treatment of bufalin with ammonium acetate in DMF solution. Their structures were elucidated by extensive spectroscopic methods. The structure of 2 was further confirmed by single-crystal X-ray diffraction analysis. Compound 1 and 2 didn't inhibit the Na+/K+-ATPase. However, both compounds showed significant inhibitory activity against the androgen dependent prostate cell LNCaP with IC50 values of 9.0 μM for 1 and 14.0μM for 2. The fact that compounds 1 and 2 inhibited the prostate cancer cells but no inhibition on Na+/K+-ATPase indicated that they might be potential anti-prostate cancer agents without the cardiac toxicity.
	TO cite this article:Xiao-Feng Yuan,Hai-Yan Tian,Juan Li, et al. A convenient way to synthesize bufadienolactam analogs with inhibitory activity against the prostate cancer cells[OL].[28 February 2013] http://en.paper.edu.cn/en_releasepaper/content/4525029


	4. Synthesis and anti-tumor activity evaluation of ent-6,7-seco-oridonin derivatives
	LI Dahong,WANG Lei,CAI Hao,WU Xiaoming,SUN Yijun,XU Jinyi
	Pharmacy 16 July 2012
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	Abstract:This paper presents the synthesis of ent-6,7-seco-oridonin derivatives from commercial available natural product oridonin (1) and their biological activities were evaluated. The results demonstrated that the most effective compound 11 has improved =anti-proliferative activity than oridonin and similar potency compared with Taxol in A549 cell and Bel-7402 cell with IC50 of 4.58 and 5.03 μM, respectively. Compound 11 was also more potent than parent compound oridonin in mice with MGC-803 gastric cancer in vivo. These results would provide valuable information in the novel anticancer drugs development.
	TO cite this article:LI Dahong,WANG Lei,CAI Hao, et al. Synthesis and anti-tumor activity evaluation of ent-6,7-seco-oridonin derivatives[OL].[16 July 2012] http://en.paper.edu.cn/en_releasepaper/content/4483740


	5. Synthesis and Biological Evaluation of Substituted Cinnamic Acid Esters as Selective MMP-2 and MMP-9 Inhibitors
	LI Nianguang,SHI Zhihao,TANG Hao,SHI Qianping,TANG Yuping
	Pharmacy 14 July 2012
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	Abstract:Substituted cinnamic acid esters with extended P1' group were synthesized under microwave irradiation and tested for their inhibitory activities on MMP-1, MMP-2 and MMP-9. Preliminary SARs analysis showed that hydroxyl groups in the benzene ring and the presence of extended spatial structures in the carboxylic acid played key roles in the MMP-2 and MMP-9 inhibitory activity and selectivity over MMP-1.
	TO cite this article:LI Nianguang,SHI Zhihao,TANG Hao, et al. Synthesis and Biological Evaluation of Substituted Cinnamic Acid Esters as Selective MMP-2 and MMP-9 Inhibitors[J].


	6. Design and synthesis of furozan-based nitric oxide-releasing derivatives of oridonin with anti-proliferative activity
	LI Dahong,WANG Lei,CAI Hao,WU Xiaoming,SUN Yijun,XU Jinyi
	Pharmacy 03 July 2012
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	Abstract:To search for novel nitric oxide (NO) releasing anti-tumor agents, a series of novel furoxan/oridonin hybrids were designed and synthesized. Firstly, the nitrate/nitrite levels in the cell lysates were tested by Griess assay and the results showed that these furoxan-based NO-releasing derivatives could produce high level of NO in vitro. Then the anti-proliferative activity of these hybrids against four human cancer cell lines were also determined, among which, 9h exhibited the most potential anti-tumor activity with IC50 values of 1.82 μM against K562, 1.81μM against MGC-803 and 0.86 μM against Bel-7402, respecively. Structure-activity relationship was concluded based on the experimental data obtained. These results suggested that NO-donor/natural product hybrids may provide a promising approach for the discovery of novel anti-tumor agents.
	TO cite this article:LI Dahong,WANG Lei,CAI Hao, et al. Design and synthesis of furozan-based nitric oxide-releasing derivatives of oridonin with anti-proliferative activity[J].


	7. Synthesis and Biological Evaluation of Heterocyclic Ring Fused Betulinic Acid Derivatives as Novel Inhibitors of Osteoclast Differentiation and Bone Resorption
	Xu Jun,Li Zhenxi,Luo Jian,Yang Fan,Liu Ting,liu Mingyao,Qiu Wen-Wei,Tang Jie
	Pharmacy 19 January 2012
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	Abstract:A series of betulinic acid (BA) derivatives were synthesized by introducing various fused heterocyclic rings at C-2 and C-3 positions. Their inhibitory effects of RANKL-induced osteoclastogenesis were evaluated by using a cell-based tartrate-resistant acid phosphatase (TRAP) activity assay. Compared with BA, most of these compounds exhibited a dramatic increase in inhibitory potency. Especially compound 20, which showed 66.9% inhibition even at low concentration of 0.1 M, was about 200-fold more potent than lead compound BA. The cytotoxicity assay on RAW264.7 suggested that the action of 20 on osteoclast differentiation was not result from its cytotoxicity. The primary mechanistic study indicated that 20 could inhibit osteoclastogenesis-related marker gene expression levels of cathepsin K and TRAP. Importantly, this compound attenuated bone loss of ovariectomy mouse in vivo. These BA derivatives could be used as potential leads for the development of a new type of antiosteoporosis agents.
	TO cite this article:Xu Jun,Li Zhenxi,Luo Jian, et al. Synthesis and Biological Evaluation of Heterocyclic Ring Fused Betulinic Acid Derivatives as Novel Inhibitors of Osteoclast Differentiation and Bone Resorption[OL].[19 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4463179


	8. A Pharmacophore Model and Database Searching for Serotonin 2A Receptor Antagonists
	FU Wei,LIU Huifang,LI Bian
	Pharmacy 06 January 2011
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	Abstract:The serotonin 2A receptor has been implicated in several neurological conditions and potent 5-HT2A antagonists have therapeutic effects in the treatment of Schizophrenia and depression. In this paper, we reported computational homology modeling of the 5-HT2A receptor based on the high-resolution X-ray structure of β2-adrenergic receptor. The accuracy of the model was validated through Procheck 3.5.4 and AutoDock 4.0 program. The antagonistic conformation of 5-HT2A was obtained by the investigation of the interaction mode of 5-HT2A with well-known potent antagonist ketanserin. The active site of the 5-HT2A receptor was mapped by five types of chemical probes by means of grid calculation. The Cluster analysis in combination with the available experimental pharmacological data was applied to guide the selection of the pharmacophore feature. Pharmacophore model was built by means of the Catalyst 4.10 and database searching was carried out on Asinex Gold Collection database, which contains ca. 200,000 molecules. As a result, 463 hits were obtained. The Lipinski's Rule of Five was used to filter out the non-drug like redundancies, the scoring function was used to rank the hits and docking study was used for the final selection. Finally, 14 molecules were selected and purchased for further biological test.
	TO cite this article:FU Wei,LIU Huifang,LI Bian. A Pharmacophore Model and Database Searching for Serotonin 2A Receptor Antagonists[OL].[ 6 January 2011] http://en.paper.edu.cn/en_releasepaper/content/4404495


	9. A Pharmacophore Model and Database Searching for Dopamine D2 Receptor Antagonists
	FU Wei,LI Bian,LIU Huifang
	Pharmacy 04 January 2011
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	Abstract:The dopamine D2 receptor (D2R) has been implicated in several neurological conditions and potent D2R antagonists have therapeutic effects in the treatment of schizophrenia and depression. In this paper, we reported computational homology modeling of the D2R based on the high-resolution X-ray structure of β2-adrenergic receptor. The accuracy of the model was validated through Procheck 3.5.4 and AutoDock 4.0 program. The active site of the D2R receptor was mapped by five types of chemical probes by means of grid calculation. The cluster analysis in combination with the available experimental pharmacological data was applied to guide the selection of the pharmacophore feature. Pharmacophore model was built by means of the Catalyst 4.10 and database searching was carried out on Asinex Gold Collection database, which contains ca. 200,000 molecules. As a result, 463 hits were obtained. The Lipinski's Rule of Five was used to filter out the non-drug like molecules, the scoring function was used to rank the hits and docking study was used for the final selection. Finally, 6 molecules were selected and purchased for further biological test.
	TO cite this article:FU Wei,LI Bian,LIU Huifang. A Pharmacophore Model and Database Searching for Dopamine D2 Receptor Antagonists[OL].[ 4 January 2011] http://en.paper.edu.cn/en_releasepaper/content/4403687


	10. Discovery of Lead Pseudopeptides for Drug Design
	Zhao Ming,Wang Yuji,Xu Yanxia,Wu Jianhui,Kang Guifeng,Peng Shiqi
	Pharmacy 04 August 2010
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	Abstract:The discovery of lead compounds is a key step to drug design. Pseudopeptide is one of the most important lead structures. Various pseudopeptides could be prepared either based on the structures or based on the action mechanisms. For the design of the anti-thrombotic, thrombolytic, anti-tumor, anti-osteoporosis and lead detoxifica- tion drugs, in the past years we published numerous pseudopeptides of alkaloid- peptides, heterocyclics-peptides, steroid-peptides, saccharide-amino acids and so on. This paper reviewed the pharmacological benefits of some pseudopeptides of our laboratory.
	TO cite this article:Zhao Ming,Wang Yuji,Xu Yanxia, et al. Discovery of Lead Pseudopeptides for Drug Design[OL].[ 4 August 2010] http://en.paper.edu.cn/en_releasepaper/content/4380631

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