Authentication email has already been sent, please check your email box: and activate it as soon as possible.
You can login to My Profile and manage your email alerts.
If you haven’t received the email, please:
|
|
There are 45 papers published in subject: > since this site started. |
Select Subject |
Select/Unselect all | For Selected Papers |
Saved Papers
Please enter a name for this paper to be shown in your personalized Saved Papers list
|
1. 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 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
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 |
2. Design, synthesis, and biological evaluation of novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase | |||
Gao Xing,Gong Haojun,Men Peng,Zhou Lu,Ye Deyong | |||
Pharmacy 06 February 2013 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
Abstract:The secretory phospholipase A2 (sPLA2) and sphingomyelin (SMS) are the key enzymes to atherosclerosis. A novel series of eight sPLA2 and SMS dual inhibitors containing indole and α-amino cyanide fragments respectively with different length carbon chain and substitution position were designed and synthesized. In vitro biological evaluation showed that all the compounds provided inhibitory effects against both SMS and sPLA2, in which, the SMS inhibitory activities were better than the positive control compound D609. The compounds 5b and 5e had moderate SMS inhibitory effects in liver homogenate and in SMS2 high expression cell homogenate respectively, as well as had ideal sPLA2 inhibitory activities. | |||
TO cite this article:Gao Xing,Gong Haojun,Men Peng, et al. Design, synthesis, and biological evaluation of novel dual inhibitors of secretory phospholipase A2 and sphingomyelin synthase[OL].[ 6 February 2013] http://en.paper.edu.cn/en_releasepaper/content/4519052 |
3. 3D-QSAR Analysis of SecA Inhibitors | |||
LI Minyong,ZHU mengyuan | |||
Pharmacy 25 January 2013 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
Abstract:SecA ATPase plays a crucial role in translocation of membrane and secreted polypeptides and proteins in bacteria and therefore a perfect target for novel antimicrobial drug design. Herein, we generated QSAR models with an alignment-independent method. The optimum model obtained for the training set was statistically significant with cross-validation regression coefficient (q2) value of 0.40 and correlation coefficient (r2) value of 0.89. These results suggest that this 3D-QSAR model can be used to guide the development of new SecA inhibitors. | |||
TO cite this article:LI Minyong,ZHU mengyuan. 3D-QSAR Analysis of SecA Inhibitors[OL].[25 January 2013] http://en.paper.edu.cn/en_releasepaper/content/4516260 |
4. Synthesis and Biological Evaluation of Caffeic Acid Amides as Selective Matrix Metalloproteinase Inhibitors | |||
LI Nianguang,SHI Zhihao,SHI Qianping,TANG Hao,TANG Yuping | |||
Pharmacy 10 September 2012 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
Abstract:A series of caffeic acid amides were synthesized, and through measurement using a fluorogenic substrate assay with human recombinant MMP-1, MMP-2 and MMP-9, compound 3f showed considerable inhibitory activities against MMP-2, MMP-9 and best selectivity over MMP-1. Prelimianay structure-activity relationship analysis indicated that caffeic acid amides with electron-donating groups at p-position of amino phenyl group showed better inhibitory activities and selectivity than those with electron-withdrawing groups. The findings of this study would provide information for the exploitation and utilization of caffeic acid as MMP inhibitor for metastatic tumour treatment. | |||
TO cite this article:LI Nianguang,SHI Zhihao,SHI Qianping, et al. Synthesis and Biological Evaluation of Caffeic Acid Amides as Selective Matrix Metalloproteinase Inhibitors[J]. |
5. 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 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
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 |
6. 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 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
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]. |
7. 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 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
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]. |
8. 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 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
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 |
9. Synthesis and Biological Evaluation of Oleanolic Acid Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B | |||
Li Hui,Zou-Hui,Gao Lixin,Liu Ting,Yang Fan,Li Jingya,Li Jia,Qiu Wen-Wei,Tang Jie | |||
Pharmacy 18 January 2012 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
Abstract:A series of oleanolic acid (OA) derivatives have been synthesized and their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Some compounds with five-membered heterocyclic ring fused at C-2, C-3 positions showed a dramatic increase in inhibition, the two most potent PTP1B inhibitors 19 (IC50 = 0.91 μM) and 21 (IC50 = 0.98 μM) showed about 3-fold more potent than lead compound OA. Some compounds with C-ring modified showed high selectivity for PTP1B over TCPTP, among them, 50 possessed the best selectivity of 6.6-fold. | |||
TO cite this article:Li Hui,Zou-Hui,Gao Lixin, et al. Synthesis and Biological Evaluation of Oleanolic Acid Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B[OL].[18 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4463053 |
10. STUDIES ON THE SYNTHESIS OF NICOTINAMIDE NUCLEOSIDE AND NUCLEOTIDE ANALOGUES AND THEIR INHIBITIONS TOWARDS CD38 NADASE | |||
CHEN Zhe,YANG Zhenjun,Zhang Liangren,LEE Hon Cheung,ZHANG Lihe | |||
Pharmacy 18 January 2012 | |||
Show/Hide Abstract | Cite this paper︱Full-text: PDF (0 B) | |||
Abstract:Nicotinamide adenine dinucleotide (NAD) analogues inhibit the NADase activity of CD38. In the current study, efficient protocols for the synthesis of substituted-nicotinamide nucleosides and nucleotides were developed. The one-pot phosphorylation-esterification strategy provides a convenient way of obtaining nicotinamide nucleoside phosphodiesters from the corresponding nucleosides. Structure-activity relationship information revealed that replacement of 3'-hydroxy group with F or N3 led to the considerably decrease of activity as compared with ara-F NMN. Phosphodiesterification of nicotinamide nucleosides lowers their inhibitory activities in some extent. | |||
TO cite this article:CHEN Zhe,YANG Zhenjun,Zhang Liangren, et al. STUDIES ON THE SYNTHESIS OF NICOTINAMIDE NUCLEOSIDE AND NUCLEOTIDE ANALOGUES AND THEIR INHIBITIONS TOWARDS CD38 NADASE[OL].[18 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4462595 |
Select/Unselect all | For Selected Papers |
Saved Papers
Please enter a name for this paper to be shown in your personalized Saved Papers list
|
About Sciencepaper Online | Privacy Policy | Terms & Conditions | Contact Us
© 2003-2012 Sciencepaper Online. unless otherwise stated