- Pharmaceutical composition for inhibiting tumor cell growth and application thereof
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The invention discloses a pharmaceutical composition for inhibiting tumor cell growth. Its effective components include M6CP-OEt, the structural formula of M6CP-OEt is shown in the description. M6CP-OEt in the pharmaceutical composition can inhibit the gr
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Paragraph 0029; 0032; 0036
(2019/06/05)
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- Glycosylated Platinum(IV) Complexes as Substrates for Glucose Transporters (GLUTs) and Organic Cation Transporters (OCTs) Exhibited Cancer Targeting and Human Serum Albumin Binding Properties for Drug Delivery
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Glycosylated platinum(IV) complexes were synthesized as substrates for GLUTs and OCTs for the first time, and the cytotoxicity and detailed mechanism were determined in vitro and in vivo. Galactoside Pt(IV), glucoside Pt(IV), and mannoside Pt(IV) were highly cytotoxic and showed specific cancer-targeting properties in vitro and in vivo. Glycosylated platinum(IV) complexes 5, 6, 7, and 8 (IC50 0.24-3.97 μM) had better antitumor activity of nearly 166-fold higher than the positive controls cisplatin (1a), oxaliplatin (3a), and satraplatin (5a). The presence of a hexadecanoic chain allowed binding with human serum albumin (HSA) for drug delivery, which not only enhanced the stability of the inert platinum(IV) prodrugs but also decreased their reduction by reductants present in human whole blood. Their preferential accumulation in cancer cells compared to noncancerous cells (293T and 3T3 cells) suggested that they were potentially safe for clinical therapeutic use.
- Ma, Jing,Wang, Qingpeng,Huang, Zhonglv,Yang, Xiande,Nie, Quandeng,Hao, Wenpei,Wang, Peng George,Wang, Xin
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p. 5736 - 5748
(2017/07/22)
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- Chemoenzymatic synthesis of ADP-d-glycero-β-d-manno-heptose and study of the substrate specificity of HldE
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An efficient one-pot three enzymes strategy for chemoenzymatic synthesis of ADP-d-glycero-β-d-manno-heptose (ADP-d, d-heptose) was reported using chemically synthesized d, d-heptose-7-phosphate and the ADP-d, d-heptose biosynthetic enzymes HldE and GmhB M
- Li, Tiehai,Wen, Liuqing,Williams, Adriel,Wu, Baolin,Li, Lei,Qu, Jingyao,Meisner, Jeffrey,Xiao, Zhongying,Fang, Junqiang,Wang, Peng George
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p. 1139 - 1147
(2014/02/14)
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- D-Glucose and d-mannose-based metabolic probes. Part 3: Synthesis of specifically deuterated d-glucose, d-mannose, and 2-deoxy-d-glucose
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Altered carbohydrate metabolism in cancer cells was first noted by Otto Warburg more than 80 years ago. Upregulation of genes controlling the glycolytic pathway under normoxia, known as the Warburg effect, clearly differentiates malignant from non-maligna
- Fokt, Izabela,Skora, Stanislaw,Conrad, Charles,Madden, Timothy,Emmett, Mark,Priebe, Waldemar
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p. 111 - 119
(2013/03/28)
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- A nonself sugar mimic of the HIV glycan shield shows enhanced antigenicity
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Antibody 2G12 uniquely neutralizes a broad range of HIV-1 isolates by binding the high-mannose glycans on the HIV-1 surface glycoprotein, gp120. Antigens that resemble these natural epitopes of 2G12 would be highly desirable components for an HIV-1 vaccine. However, host-produced (self)-carbohydrate motifs have been unsuccessful so far at eliciting 2G12-like antibodies that cross-react with gp120. Based on the surprising observation that 2G12 binds nonproteinaceous monosaccharide D-fructose with higher affinity than D-mannose, we show here that a designed set of nonself, synthetic monosaccharides are potent antigens. When introduced to the terminus of the D1 arm of protein glycans recognized by 2G12, their antigenicity is significantly enhanced. Logical variation of these unnatural sugars pinpointed key modifications, and the molecular basis of this increased antigenicity was elucidated using high-resolution crystallographic analyses. Virus-like particle protein conjugates containing such nonself glycans are bound more tightly by 2G12. As immunogens they elicit higher titers of antibodies than those immunogenic conjugates containing the self D1 glycan motif. These antibodies generated from nonself immunogens also cross-react with this self motif, which is found in the glycan shield, when it is presented in a range of different conjugates and glycans. However, these antibodies did not bind this glycan motif when present on gp120.
- Doores, Katie J.,Fulton, Zara,Hong, Vu,Patel, Mitul K.,Scanlan, Christopher N.,Wormald, Mark R.,Finn,Burton, Dennis R.,Wilson, Ian A.,Davis, Benjamin G.
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scheme or table
p. 17107 - 17112
(2011/02/25)
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- Regio- and chemoselective reductive cleavage of 4,6-O-benzylidene-type acetals of hexopyranosides using BH3·THF-TMSOTf
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Benzylidene-type cyclic acetals of carbohydrates undergo efficient reductive ring opening using BH3·THF and a catalytic amount of TMSOTf at room temperature. 4,6-O-Benzylidene-hexopyranosides afford the corresponding 4-O-benzyl ethers exclusive
- Daragics, Katalin,Fügedi, Péter
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experimental part
p. 2914 - 2916
(2009/09/06)
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- Highly efficient chemoenzymatic synthesis of naturally occurring and non-natural α-2,6-linked sialosides: A P. damsela α-2,6- sialyltransferase with extremely flexible donor-substrate specificity
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(Chemical Equation Presented) Just relax: A one-pot, three-enzyme chemoenzymatic synthetic approach is highly efficient for obtaining complex sialosides that contain diverse naturally occurring sialic acid modifications. α-2,6-Linked sialosides containing
- Yu, Hai,Huang, Shengshu,Chokhawala, Harshal,Sun, Mingchi,Zheng, Haojie,Chen, Xi
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p. 3938 - 3944
(2007/10/03)
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- Chemical synthesis of a hexasaccharide comprising the Lewis(x) determinant linked β-(1→6) to a linear trimannosyl core and the precursor pentasaccharide lacking fucose
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Phenyl 2,3,4-tri-O-acetyl-6-O-chloroacetyl-1-thio-α,β-mannopyranoside (5) was condensed with benzyl O-(2,3,4-tri-O-benzyl-β-D-mannopyranosyl)-(1→6)-2,3,4-tri-O-benzyl-α -D-mannopyranoside (12) in the presence of NIS-triflic acid to give, after removal of the chloroacetyl group, the key intermediate, benzyl O-(2,3,4-tri-O-acetyl-α-D-mannopyranosyl)-(1→6)-O-(2,3,4-tri-O-benzy l-β-D-mannopyranosyl)-(1→6)-2,3,4-tri-O-benzyl-α-D-mannopyranoside (14). A similar condensation of 6 and 7 with acceptor 14, followed by the removal of protecting groups, afforded 16 and 18, respectively. These compounds are expected to be useful in specificity studies of an antibody raised against a related, synthetic antigen that we are recurrently investigating.
- Jain,Matta
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p. 101 - 111
(2007/10/03)
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- NEW SYNTHESES OF D- AND L-GLYCERO-D-MANNO-HEPTOSES
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Three methods for the synthesis of the title compounds starting from benzyl 2,3,4-tri-O-benzyl-α-D-manno-hexodialdo-1,5-pyranoside (7) have been elaborated.Conversion of 7 into the cyanohydrin followed by reduction to give the amine and then deamination gave a derivative of L-glycero-D-manno-heptose in low yield.Condensation of 7 with 2-methylfuran gave two stereoisomeric 6-C-(2-methyl-5-furyl) derivatives.The preponderant stereoisomer was ozonised and then reduced to give a derivative of D-glycero-D-manno-heptose.Condensation of 7 with allyloxymethylmagnesium chloride gave derivatives of both heptoses in good yield and with an L-glycero-D-glycero ratio of 3.2:1.Deprotection of these derivatives gave the heptoses in high yield.
- Dziewiszek, Krzysztof,Zamoiski, Aleksander
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p. 163 - 172
(2007/10/02)
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