A new application about 10343-06-3

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Glucoside derivatives of podophyllotoxin: Synthesis, physicochemical properties, and cytotoxicity

Background: Widespread concern of the side effects and the broad-spectrum anticancer property of podophyllotoxin as an antitumor agent highlight the need for the development of new podophyllotoxin derivatives. Although some per-butyrylated glucosides of podophyllotoxin and 4beta-triazolyl-podophyllotoxin glycosides show good anticancer activity, the per-acetylated/free of podophyllotoxin glucosides and their per-acetylated are not well studied. Methods: A few glucoside derivatives of PPT were synthesized and evaluated for their in vitro cytotoxic activities against five human cancer cell lines, HL-60 (leukemia), SMMC-7721 (hepatoma), A-549 (lung cancer), MCF-7 (breast cancer), and SW480 (colon cancer), as well as the normal human pulmonary epithelial cell line (BEAS-2B). In addition, we investigated the structure?activity relationship and the physicochemical property?anticancer activity relationship of these compounds. Results: Compound 6b shows the highest cytotoxic potency against all five cancer cell lines tested, with IC50 values ranging from 3.27¡À0.21 to 11.37¡À0.52 muM. We have also found that 6b displays higher selectivity than the etoposide except in the case of HL-60 cell line. The active compounds possess similar physicochemical properties: MSA > 900, %PSA < 20, ClogP > 2, MW > 700 Da, and RB > 10. Conclusion: We synthesized several glucoside derivatives of PPT and tested their cytotoxicity. Among them, compound 6b showed the highest cytotoxicity. Further studies including selectivity of active compounds have shown that the selectivity indexes of 6b are much greater than the etoposide except in the case of HL-60 cell line. The active compounds possessed similar physicochemical properties. This study indicates that active glucoside analogs of podophyllotoxin have potential as lead compounds for developing novel anticancer agents.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Brief introduction of 951127-25-6

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A dipeptidyl peptidase – IV inhibitors (by machine translation)

The invention provides general formula (I) amino-tetrahydropyran derivatives, their pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, and its preparation method and comprise the compound of the pharmaceutical composition. The compound can inhibit the dipeptidyl peptidase IV (DPP – IV) activity, can be used for treating diseases associated with dipeptidyl peptidase IV, in particular to the treatment of diabetes. (by machine translation)

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Discovery of 10343-06-3

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A useful and convenient synthetic procedure for hydrolysis of thioglycosides

Various thioglycosides 1 are smoothly hydrolyzed chemo-selectively to the corresponding 1-hydroxy sugars 2 in good yields at 0-5C by employing (NH4)6Mo7O24¡¤ 4H2O-H2O2 or H2MoO4¡¤H2O-H2O2 to promote oxidation of ammonium bromide in the presence of perchloric acid in CH2Cl2-H2O solvent system. Mild conditions, good yields, no side reactions such as bromination either at the anomeric position or double bond, and even oxidation at the sulfur are some of the major advantages.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Synthesis of novel 10,11-methylenedioxy-camptothecin glycoside derivatives and investigation of their anti-tumor effects in vivo

10,11-Methylenedioxy-camptothecin (FL118) is a novel camptothecin analogue that possesses exceptional antitumor efficacy in human tumor xenograft models. The aim of the current study was to develop novel 20-substituted FL118 derivatives coupled with glycosyl-succinic acid esters with improved antitumor efficacy. These FL118 glycoside derivatives were designed, synthesized and their cytotoxicity evaluated in three tumor cell lines (A-549, MDA-MB-231 and RM-1). All of the derivatives showed superior in vitro cytotoxic activity and were more potent than irinotecan in A549 and MDA-MB-231 cells. In mouse prostate cancer cells RM-1, 10,11-methylenedioxy-camptothecin rhamnoside 11b displayed significant activities with IC50 of 48.27 nM. Western blot analysis demonstrated that 11b inhibited survivin expression and induced cancer cells apoptosis. Further cell cycle analyses clearly showed 11b induced G2/M phase cell cycle arrest. Molecule docking studies suggested that the binding mode of 11b was different from that of the crystal complex of ligand topotecan in Top1/DNA. Importantly, 11b showed high in vivo antitumor efficacy in the RM-1 mouse model with transplantation of prostate cancer (TGI = 44.9%) at dose of 9 mg kg?1 without apparent toxicity.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Archives for Chemistry Experiments of 34213-34-8

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Synthetic Route of 34213-34-8, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 34213-34-8, Name is Methyl 2,3,4-Tri-O-acetyl-b-D-glucuronic Acid Methyl Ester, molecular formula is C14H20O10. In a Article£¬once mentioned of 34213-34-8

Synthesis and Antitubercular, Antimicrobial, and Hemolytic Activity of Methyl D-Glucopyranuronate and Its Simplest Derivatives

Methyl glucuronate and some of its simplest derivatives have been synthesized, and their antitubercular, antimicrobial, and hemolytic activities have been studied. The simplest derivatives of glucuronic acid have been shown for the first time to exhibit a high antitubercular activity which is comparable with the activity of isoniazid.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Can You Really Do Chemisty Experiments About 499-40-1

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.499-40-1, Name is (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal, molecular formula is C12H22O11. In a Article£¬once mentioned of 499-40-1, Quality Control of: (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal

The crystal packing of bis(2,2?-dipyridylamido)cobalt(II), Co(dpa)2, is stabilized by C-H…N bonds: Are there any real precedents?

A crystallographic study of Co(dpa)2 reveals that the pseudo-tetrahedral molecules stack together to form a one-dimensional ribbon with the molecules linked together through significant C-H…N interactions; the C…N separation is 3.41(3) A and the angle at the hydrogen atom is 177(2).

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

More research is needed about 73464-50-3

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ANTI-CD98 ANTIBODIES AND ANTIBODY DRUG CONJUGATES

The invention relates to anti-CD98 antibodies and antibody drug conjugates (ADCs), including compositions and methods of using said antibodies and ADCs.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Unexpected helicity control and helix inversion: Homochiral helical nanotubes consisting of an achiral ligand

The ligand tppda has been designed and synthesized as molecular leverage for helicity control when reacted with Cd2+ ions. The guests MeOH or DMF preferentially stabilize the P-helical isomer, while the guest H 2O causes a helix inversion to give the M-helical isomer as the major isomer without any chiral auxiliary.

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Tetrahydropyran – Wikipedia,
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Influence of supramolecular bonding contacts on the spin crossover behaviour of iron(ii) complexes from 2,2?-dipyridylamino/s-triazine ligands

Reactions of the related ligands 2-(N,N-bis(2-pyridyl)amino)-4,6- bis(phenoxy)-(1,3,5)triazine (L1) and 2-(N,N-bis(2-pyridyl)amino)-4,6- bis(pentafluorophenoxy)-(1,3,5)triazine (L1F) with iron(ii) thiocyanate produced two spin-crossover coordination compounds with distinct cooperative behaviours. trans-[Fe(L1)2(NCS)2] ¡¤2CH2Cl2 (1) displays a very gradual transition centred at T = 233 K, characterized by a DeltaT80 (namely the temperature range within which 80% of the transition considered occurs) of 90 K, while that of fluorinated trans-[Fe(L1F)2(NCS) 2]¡¤2CH3CN (3) is significantly more abrupt (and centred at T = 238 K), with a DeltaT80 of 50 K, resulting from supramolecular contacts induced by the fluorinated phenol groups. The coordination compound equivalent to 1 with selenocyanate anions, namely trans-[Fe(L1)2(NCSe)2]¡¤4CH2Cl 2¡¤4CH3OH (2), also exhibits SCO properties centred at T = 238 K, but the transition is very gradual (DeltaT80 = 150 K). Light-induced excited spin-state trapping (LIESST) is effective although incomplete for 2 and 3, while it is complete with a TLIESST of 58 K for 1. The Royal Society of Chemistry 2013.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of 499-40-1

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Crystal structure of a new triply-bridged cobalt(III) dimer with 2,2?-dipyridylamine (dipyam), [Co2(mu-OH)2 (mu-OAc)(OAc)2(dipyam)2]AcO¡¤EtOH

The structure of [Co2(mu-OH)2(mu-OAc)(OAc) 2(dipyam)2]-AcO¡¤EtOH (1) has been determined by single-crystal X-ray analysis. The cationic complex may be described as a “di(mu-hydroxo)(mu-acetato)dicobalt(III)” core with chelating 2,2″-dipyridylamine and monodentate acetate ligands. The coordination polyhedron around each cobalt atom is a distorted octahedral. The dimers are linked in the crystal by N-H…Oionic AcO and C-H…Omonodentate AcO hydrogen bonds. Spectroscopic data are also presented.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics