摘要：Poly （hydroxyethyl, octanediamine）-DL-aspartamide （PHOA） hydrogels were prepared by adding mixture of 1,8-octanediamine and ethanolamine to PA in DMF at room temperature. The properties of the hydrogels were investigated by FT-IR,^1 HNMR, TGA and cell culture assay.

摘要：A series of 7-azaindol derivatives were designed based on the homologous 3D model of human *** compounds were synthesized and evaluated for their human acrosin inhibitory activities in *** 7a,7i,7j,7k and 7n showed highly inhibitory activity against human *** three-dimensional structure-activity relationship was investigated through a CoMFA model,which provided valuable information to further study of potential human acrosin inhibitors.

摘要：Novel chiral tetralin compounds were designed and synthesized, and their antifungal activities in vitro were tested. The results showed that all of target compounds had potent antifungal activities, and were stronger than that of control compounds tetrahydroisoquinolines. The binding model of lead molecules in the active site of CYP51 of Candida albicans showed that lead compound specifically interacted with the amino acids residues in the active site, without binding with the heme of CYP51, which was different from azole antifungal drugs. The present study might afford a novel lead molecule to develop non-azole CYP51 inhihitars of fungi.

摘要：A series of 1-（1H-1,2,4-triazole-1-yl）-2-（2,4-difluoropheny1）-3-（N-isoproy1-N-substituted-amino）-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase （CYP51）. Their structures were confirmed by MS and ^1H NMR. In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi. The results showed that all title compounds exhibited activity against fungi tested to some extent. Compounds 3c, 3d, 7a, 7b and 7e exhibited more potent antifungal activities against nearly all fungi tested except AspergiUus fumigatus than fluconazole. ？2009 Qiu Ye Wu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All fights reserved.

摘要：Metal-based secondary building unit and the shape of organic ligands are the two crucial factors for determining the final topology of metal-organic materials.A careful choice of organic and inorganic structural building units occasionally produces unexpected structures,facilitating deeper fundamental understanding of coordination-driven self-assembly behind metal-organic ***,we have synthesized a triangular metal-organic polygon(MOT-1),assembled from bulky tetramethyl terephthalate and Zr-based secondary building ***,the Zr-based secondary building unit serves as an unusual ditopic Zr-connector,toform metal-organic polygon MOT-1,proven to be a good candidate for water adsorption with *** study highlights the interplay of the geometrically frustrated ligand and secondary building unit in controlling the connectivity of metal-organic *** a strategy can be further used to unveil a new class of metal-organic materials.

摘要：Based on the active site of lanosterol 14α-demethylase of azole antifungal agents,sixteen 1-（1H-1,2,4-triazole-1-yl）- 2-（2,4- difluorophenyl）-3-（N-n-butyl-N-1-substitutedbenzyl-4-methylene-1H-1,2,3-triazole）-2-propanols have been designed,synthesized and evaluated as antifungal *** of preliminary antifungal tests against eight human pathogenic fungi in vitro showed that some of the compounds exhibited excellent activities with broad spectrum.

摘要：Eight new water-soluble amino acid conjugates 6 a-h of chlorin p6 ethers(5 a-d) were synthesized and preliminarily investigated for their in vitro PDT antitumor activity and structure-activity relationship(SAR). The results showed that all compounds exhibited much higher phototoxicity against tumor cells than talaporfin. SAR analysis indicated that PDT antitumor effect enhanced with the increase of carbon chain length of alkoxyl ether bonds at 3~1-position, and L-aspartic acid was superior to L-glutamic acid. In particular, the IC_50 values of most phototoxic compound 6 d were 0.20 mmol/L against A549 cell and0.41υmmol/L against B16-F10 cell, which individually represented 31-and 24-fold increase of antitumor potency compared to talaporfin, suggesting that it was a promising candidate photosensitizer(PS) for PDT applications due to its strong absorption at long wavelength, high phototoxicity, low dark cytotoxicity and good water-solubility.

摘要：Drug resistance is a great challenge in cancer therapy using chemotherapeutic agents. Administration of these drugs with siRNA is an efficacious strategy in this battle. Here, the present study tried to incorporate siRNA and paclitaxel(PTX) simultaneously into a novel nanocarrier. The selectivity of carrier to target cancer tissues was optimized through conjugation of folic acid(FA) and glucose(Glu) onto its surface. The structure of nanocarrier was formed from ternary magnetic copolymers based on FeCopolyethyleneimine(FeCo-PEI) nanoparticles and polylactic acid-polyethylene glycol(PLA-PEG) gene delivery system. Biocompatibility of FeCo-PEI-PLA-PEG-FA(NPsA), FeCo-PEI-PLA-PEG-Glu(NPsB) and FeCo-PEI-PLA-PEG-FA/Glu(NPsAB) nanoparticles and also influence of PTX-loaded nanoparticles on in vitro cytotoxicity were examined using MTT assay. Besides, siRNA-FAM internalization was investigated by fluorescence microscopy. The results showed the blank nanoparticles were significantly less cytotoxic at various concentrations. Meanwhile, siRNA-FAM/PTX encapsulated nanoparticles exhibited significant anticancer activity against MCF-7 and BT-474 cell lines. NPsAB/siRNA/PTX nanoparticles showed greater effects on MCF-7 and BT-474 cells viability than NPsA/siRNA/PTX and NPsB/siRNA/***, they induced significantly higher anticancer effects on cancer cells compared with NPsA/siRNA/PTX and NPsB/siRNA/PTX due to their multi-targeted properties using FA and Glu. We concluded that NPsAB nanoparticles have a great potential for co-delivery of both drugs and genes for use in gene therapy and chemotherapy.

摘要：Two series of 1-（benzoxazole-2-yl）piperazine （Sa-i） and 4-（benzoxazole-2-yl）piperidine compounds （10a-i） were designed, synthesized and evaluated for their α1-AR antagonistic activities. Biological assay in vitro indicated that 10h showed slightly stronger α1-AR antagonistic activity to that of our lead compound 1.

摘要：A number of novel 2-（2-arylmorpholino-4-yl）ethyl 1-（4-chlorobenzoyl）-5-methoxy-2-methyl-lH-indol-3- acetate hydrochlorides were synthesized and tested for their cyclooxygenase （COX-1 and COX-2） inhibition prop- erties in vitro. Many of these compounds exhibited moderate to good selective COX-2 inhibition, and subtle struc- tural changes in the substituents on the side chain of the ester moiety altered the inhibitory properties significantly. 2-[2-（4-Butoxyphenyl）morpholino-4-yl]ethyl 1-（4-chlorobenzoyl）-5-methoxy-2-methyl-IH-indol-3-acetate hydro- chloride （If）, showed good selective COX-2 inhibitory activity （Selective index （SI） 182）, which is comparative with celecoxib （SI 214）, a COX-2 inhibitor of diarylpyrazoles. While 2-[2-（2,4-dichloro-5-fluorophenyl）mor- pholino-4-yl]ethyl 1-（4-chlorobenzoyl）-5-methoxy-2-methyl-IH-indol-3-acetate hydrochloride （lg）, showed greater selective COX-2 inhibitory activity （SI 358） than celecoxib. Both compounds were identified as compromising de- rivatives in this class to reduce the side effects generated by nonsteroidal anti-inflammatory drugs （NSAIDs） indo- methacin.