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	1. 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


	2. 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


	3. Synthesis, Characterization, and Crystal Structures of Propargyl Naphthalimides
	PENG Li-Ping,LV Jing-Song,ZHOU Cheng-He
	Pharmacy 26 February 2014
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	Abstract:Two title molecules, 6-bromo-2-(prop-2-ynylamino)-1H-benzo[de]isoquinoline -1,3(2H)-dione (4) and 6-bromo-2-(diprop-2-ynylamino)-1H-benzo[de]isoquinoline-1,3(2H)-dione (5), were synthesized and characterized by single-crystal X-ray diffraction, IR, 1H NMR, MS, fluorescence spectra, and powder X-ray diffraction (PXRD). The structure of crystal 4 (CCDC 981232) belongs to the triclinic system, space group P-1 with a = 7.5827(5), b = 7.8886(6), c = 10.5217(7) ?, α = 96.368(6), β = 90.223(5), γ = 92.353(6)o, V = 624.95(7) ?3, Dc = 1.749 g/cm3, μ = 4.52 mm-1, F(000) = 328, Rint = 0.0260, R (I > 2σ(I)) = 0.0622, wR (I > 2σ(I)) = 0.1454, R (all data) = 0.0683 and wR (all data) = 0.1484. In this crystal, a 2D layer supramolecular network structure was formed through hydrogen bonds of N(2)?H(2)oooO(1) and C(15)?H(15)oooO(1), and the Br atom was disordered over two positions with refined occupancies of 0.8589(3) and 0.1410(7). The calculated bond lengths and bond angles of compound 4 were consistent with the result of crystallography. Fluorescence properties of compounds 4 and 5 in different solvents were also studied. Moreover, the two synthesized compounds 4 and 5 were screened for their antimicrobial activities against seven bacteria and four fungi. Bioactive assay manifested that the two compounds exhibited moderate antibacterial and antifungal activities against the tested strains in comparison with the reference drugs norfloxacin, chloromycin and fluconazole.
	TO cite this article:PENG Li-Ping,LV Jing-Song,ZHOU Cheng-He. Synthesis, Characterization, and Crystal Structures of Propargyl Naphthalimides[OL].[26 February 2014] http://en.paper.edu.cn/en_releasepaper/content/4587490


	4. Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents
	LIU Zheng,LI Wei,QIN Kai,WEN Kan,ZHU Chenjian,LI Nianguang,BIAN Huimin,WEN Hongmei,CHEN Long
	Pharmacy 18 April 2013
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	Abstract:Liguzinediol (LZDO) could mediate the positive inotropic effects through sarcoplasmic reticulum Ca2+ ATPase-dependent mechanism without the risk of arrhythmia. However, the pharmacophore of LZDO contributed to the activities was not clear. The aim of this work is to explore the relationship between positive inotropic effect and scaffold of LZDO as well as to check whether the pharmacophore of LZDO on anti-heart failure activity was located at the pyrazine ring. A series of LZDO analogs (3a-b, 4a-b, 9-19) were designed and synthesised, and their activities were evaluated on isolated heart contractility by Langendorff perfusion. The results showed that the efficacy of LZDO was reduced when the hydroxyl, carboxyl or ester moieties at the side chain position of LZDO were induced, and the para-dihydroxy in LZDO was necessary for its activity. Thus, the pharmacophore of positive inotropic effect might be located at the whole scaffold of LZDO, but not at the pyrazine ring. The finding may provide important clue of pharmacophore for the development of novel cardiotonic agents.
	TO cite this article:LIU Zheng,LI Wei,QIN Kai, et al. Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents[OL].[18 April 2013] http://en.paper.edu.cn/en_releasepaper/content/4538513


	5. Spectral, Mathematical and Electrophoretic Models for Anti-tumor Activity Evaluation and Intercalation Mechanism Investigation of Small Molecules
	XU Yanxia,ZHAO Ming,ZHANG Xiaoyi,WANG Yuji,WU Jianhui,HU Fei,ZHANG Jianwei,PENG Shiqi
	Pharmacy 24 February 2011
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	Abstract:For improving the cancer chemotherapy the discovery of new DNA intercalators is one of the effective approaches. The investigations have demonstrated the utility of the models in both anti-tumor activity evaluation and the intercalation mechanism identification. This paper described the DOCK score, ultraviolet (UV), fluorescence, circular dichroism (CD), relative viscosity, melting curve, kinetics in CT DNA sta- cking of small molecule intercalator, kinetics in CT DNA intercalation of small mole- cule intercalator, interaction stabilizing the stacking complex of small molecule inter- calator and CT DNA and the gel electrophoresis based models as well as their use in the identification of small molecule intercalating towards DNA.
	TO cite this article:XU Yanxia,ZHAO Ming,ZHANG Xiaoyi, et al. Spectral, Mathematical and Electrophoretic Models for Anti-tumor Activity Evaluation and Intercalation Mechanism Investigation of Small Molecules[OL].[24 February 2011] http://en.paper.edu.cn/en_releasepaper/content/4412178


	6. Fluroscence-based assay to calculate dissociation rate constant of β-secretase (BACE1) inhibitors
	ZHAO Ying
	Pharmacy 17 February 2011
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	Abstract:β-secretase (BACE1) is one of the potential drug target for Alzheimer's Disease (AD). The ideal clinically available BACE1 inhibitors should have some features, such as good effect, low dose and high selectivity. The dissociation rate constant (Koff) is useful to predict the selectivity of a BACE1 inhibitor. Based on the common used fluorescent inhibitory activity measurement, we developed the assay to measure Ki and Kon of BACE1 inhibitor, and calculated Koff using the relationship of Ki = Koff / Kon. In our assay, a tight-binding inhibitor of BACE1, OM99-2, was measured to have the Koff of 9.54×10-4 S-1, which is in good accordance with previous literature. This assay is economic and simple to use, providing a rapid way for Koff measurement of BACE1 inhibitors, which may further contribute to SAR studies.
	TO cite this article:ZHAO Ying. Fluroscence-based assay to calculate dissociation rate constant of β-secretase (BACE1) inhibitors[OL].[17 February 2011] http://en.paper.edu.cn/en_releasepaper/content/4411026

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