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There are 45 papers published in subject: > since this site started. |
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1. Discovery of quercetin derivatives as metal ions chelators with potent anti-HCV activities | |||
ZHONG Dongwei,LIU Mingming,CAO Yang,ZHOU Lu,YE Deyong | |||
Pharmacy 08 May 2017 | |||
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Abstract:The α,γ-diketoacid (DKA) analogues or isosteres show potent inhibition of hepatitis C virus (HCV) NS5B polymerase through chelation of the two magnesium ions at the active site. The anti-HCV activity of flavonoid quercetin (2) could partly be attributed to its structural mimic of DKAs. In order to delineate the structural features required for the inhibitory effect and improve the anti-HCV potency, two novel quercetin analogues, 7-O-arylmethyl quercetin and quercetin-3-O-benzoic acid-ester, were designed, synthesized and evaluated for their anti-HCV properties in cell-based assays. Among the 38 newly synthesized compounds, 7-O-substituted derivative 3i and 3-O-substituted derivative 4f were found to be the most active in corresponding series (EC50 = 3.8 μM and 9.0 μΜ, respectively). Docking studies suggested that the quercetin analogues are capable of establishing key coordination with the two magnesium ions as well as interactions with residues at the active site of HCV NS5B. | |||
TO cite this article:ZHONG Dongwei,LIU Mingming,CAO Yang, et al. Discovery of quercetin derivatives as metal ions chelators with potent anti-HCV activities[OL].[ 8 May 2017] http://en.paper.edu.cn/en_releasepaper/content/4730625 |
2. Tetrazole and triazole as bioisosteres of carboxylic acid: discovery of diketo tetrazoles and diketo triazoles as anti-HCV agents | |||
SONG Wuhui,LIU Mingming,ZHONG Dongwei,YE Deyong,ZHOU Lu,YUAN Zhenghong | |||
Pharmacy 28 April 2017 | |||
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Abstract:In this paper, a series of diketo tetrazoles and diketo triazoles were designed and synthesized as bioisosteres of α, γ-diketo acid, the active site inhibitor of HCV (Hepatitis C virus) polymerase NS5B. Among the synthesized compounds, 4-(4-fluorobenzyloxy)phenyl diketo triazole (30) exhibited anti-HCV activity with an EC50 value of 3.9 μM and an SI value more than 128. The reduction of viral protein and mRNA levels were also validated, supportingthe anti-HCV activity of compound 30. These results provide convincing evidence that the diketo tetrazoles and diketo triazoles can be developed as bioisosteres of α,γ-diketo acid to exhibit potent inhibitory activity against HCV. | |||
TO cite this article:SONG Wuhui,LIU Mingming,ZHONG Dongwei, et al. Tetrazole and triazole as bioisosteres of carboxylic acid: discovery of diketo tetrazoles and diketo triazoles as anti-HCV agents[OL].[28 April 2017] http://en.paper.edu.cn/en_releasepaper/content/4730608 |
3. The synthesis and biological evaluation of Targeted Peptide conjugate of phthalocyanine | |||
Zhangyong Hong,Zhixiong Zeng,Fu Li | |||
Pharmacy 25 December 2015 | |||
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Abstract:In recent decades, photodynamic therapy has been rapid developed. In the process of photodynamic therapy, photosensitizer plays a vital role. Here we reported our synthestic studies and activitiy test of two new peptide conjugates zinc phthalocyanine photosensitizers for targeted cancer ohotodynamic therapy, Synthesis asymmetric phthalocyanine PCZN2 by introducing glycol structure and asymmetric phthalocyanine PCZN5 by introducing a hydrophilic group hydroxyl. By introducing hydrophilic functional groups, it can greatly increase the solubility of phthalocyanine. The two highly soluble phthalocyanine PCZN2 and phthalocyanine PCZN5By were conjugated to EGFR targeting peptide D4 on resin through solid phase synthesis, which solve the problem of separation and purification about phthalocyanine coupled. Optical experiments show the product has a high quantum yield and singlet oxygen yield. The maximum absorption wavelength is at 685nm with good penetration depth. Cytotoxicity test (MTT) showed targeting peptide conjugate phthalocyanine PCZN3 and PCZN6 are toxic selectively to tumor cells. Confocal microscopic experiments showsed they are able to be selectively recognized by tumor cells. In vivo imaging show both materials PCZN3 and PCZN6 are able to concentrate in tumors in mice with strong targeting. These new targeting photosensitizers show good potential for cancer photodynamic therapy. | |||
TO cite this article:Zhangyong Hong,Zhixiong Zeng,Fu Li. The synthesis and biological evaluation of Targeted Peptide conjugate of phthalocyanine[OL].[25 December 2015] http://en.paper.edu.cn/en_releasepaper/content/4669782 |
4. Cyathane Diterpenoids of Macrofungi | |||
YIN Xia,CAO Chenyu,GAO Jinming | |||
Pharmacy 31 August 2015 | |||
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Abstract:Cyathane diterpenoids, occurring exclusively in higher mushrooms, represent an important class of secondary metabolites, possessing a characteristic 5/6/7 tricyclic carbon scaffold. These compounds show a diverse range of biological activities, such as antimicrobial, anti-MRSA, agonistic toward the kappa-opioid receptor, anti-inflammatory, anti-proliferative and NGF-like properties. This review, citing 96 references, summarises their chemistry and bioactivities of cyathane diterpenoids isolated from higher mushrooms in the last four decades, to illustrate the chemo-diversity and biological significance of these diterpenoids. | |||
TO cite this article:YIN Xia,CAO Chenyu,GAO Jinming. Cyathane Diterpenoids of Macrofungi[OL].[31 August 2015] http://en.paper.edu.cn/en_releasepaper/content/4653605 |
5. Crystal Structure and New Polymorphic Forms of Lorcaserin Hydrochloride | |||
LIU Song,ZHOU Mengqing,GU Jiali,GAO Haitao,ZHANG Guoqing | |||
Pharmacy 08 July 2015 | |||
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Abstract:With the recrystallization method, a new lorcaserin hydrochloride form has been prepared, and compared with the original form. The two forms had been analyzed by using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), and scanning electron microscopy (SEM). The new form was confirmed exist, and it is different from t the original form. This is the first report about the lorcaserin hydrochloride new form . | |||
TO cite this article:LIU Song,ZHOU Mengqing,GU Jiali, et al. Crystal Structure and New Polymorphic Forms of Lorcaserin Hydrochloride[OL].[ 8 July 2015] http://en.paper.edu.cn/en_releasepaper/content/4649729 |
6. Aldehyde Mediated Nitrosation of Amino Acid | |||
YANG Yue,LIU Zhiying,ZHANG Fang,TANG Erqing,DUAN Jianli | |||
Pharmacy 09 June 2015 | |||
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Abstract:Everyday humans consume significant quantities of amino acids and sugars. Sugars are the major source of dietary aldehydes. Imines could be produced from the reaction between the amino acid and the sugars under gastric conditions and a possible N-nitroso Amadori comound product could be formed in the endogenous nitrosation process of imines. In this study, nitrosation of the imine salt 19 has been demostrated under the simulated gastric conditions. The resulting N-nitroso Amadori compound 11 was isloated by column chromatography and the 1H NMR and 13C NMR are identical with the standard compound. | |||
TO cite this article:YANG Yue,LIU Zhiying,ZHANG Fang, et al. Aldehyde Mediated Nitrosation of Amino Acid[OL].[ 9 June 2015] http://en.paper.edu.cn/en_releasepaper/content/4646252 |
7. Studies Towards The Synthesis of N-nitrosolactones | |||
LIU Miao,LI Shanshan,CHENG Shuang,DUAN Jianli | |||
Pharmacy 07 May 2015 | |||
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Abstract:TBS protected 3-β-azido-lactone is a very useful synthetic intermediate for the total synthesis of C-arylglycosides and other related compounds.Actually ,The 3-β-azido-lactone can be synthetized by a very route and highly stereoselective way in high yields.????? | |||
TO cite this article:LIU Miao,LI Shanshan,CHENG Shuang, et al. Studies Towards The Synthesis of N-nitrosolactones[OL].[ 7 May 2015] http://en.paper.edu.cn/en_releasepaper/content/4641141 |
8. 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 |
9. The Design of Pegylated Anticancer Drugs | |||
WANG Jinqiang,SHEN Youqing | |||
Pharmacy 04 January 2015 | |||
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Abstract:Poly (ethylene oxide) was a water soluble non-immunological compound often used for preparation of polymer-conjugated drugs. High molecular weight PEG (>20 KDa) was used to dissolve drugs in water and prolong the circulating time in vivo. Linear and dentritic PEG-drug conjugate was developed to achieve the best in vivo result. In addition, low molecular weight PEG (<20 KDa) have also been used to increase water solubility in the form of nanoparticles and to introduce non-immunological property to prolong the circulating time. As described ind published reviews, the pegylated drugs were mainly focused on high molecular PEG, and most clinic or pre-clinic PEG-drugs followed this formulation. However, due to the development of nano-technology, pegylated nano-particles have also gone into pre- or clinic research. So it is necessary to have a whole introduction of this area. We will divided this area by the structure of the compounds and the drug. In the interest of brievity, we would mainly describe the anti-cancer small molucular compound drug, and protein would not be included in the review. | |||
TO cite this article:WANG Jinqiang,SHEN Youqing. The Design of Pegylated Anticancer Drugs[OL].[ 4 January 2015] http://en.paper.edu.cn/en_releasepaper/content/4626589 |
10. Facile synthesis and cytotoxicity of 1'(N)-acetic acid esters of 20(S)-camptothecins | |||
LI Dizao | |||
Pharmacy 09 September 2014 | |||
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Abstract:A series of novel 1'(N)-acetic acid esters of 20(S)-camptothecins (CPTs) have been synthesized and all of the esters were assayed for in vitro cytotoxicity against five human cancer cell lines A549, Bel7402, BGC-823, HCT-8 and A2780. The results showed that most of the assayed compounds exhibited good antiproliferative activity on these tumor cell lines. Here the synthesis and the in vitro antitumor evaluation of 20-O-linked substituted 1'(N)-acetic acid ester derivatives of CPTs are reported. | |||
TO cite this article:LI Dizao. Facile synthesis and cytotoxicity of 1'(N)-acetic acid esters of 20(S)-camptothecins[OL].[ 9 September 2014] http://en.paper.edu.cn/en_releasepaper/content/4608374 |
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