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p53-Murine double minute 2 (MDM2) interaction and histone deacetylases (HDACs) are important targets in antitumor drug development. Inspired by the synergistic effects between MDM2 and HDACs, the first MDM2/HDACs dual inhibitors were identified, which showed excellent activities against both targets. In particular, compound 14d was proven to be a potent and orally active MDM2/HDAC dual inhibitor, whose antitumor mechanisms were validated in cancer cells. Compound 14d showed excellent in vivo antitumor potency in the A549 xenograft model, providing a promising lead compound for the development of novel antitumor agents. Also, this proof-of-concept study offers a novel and efficient strategy for multitargeting antitumor drug discovery.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2971-79-1, molcular formula is C7H13NO2, introducing its new discovery. Recommanded Product: 2971-79-1

The invention relates to a dihydropyrimidine compounds and their use as medicaments, in particular as the treatment and prevention of hepatitis b in drug use. In particular, the invention relates to the general formula (I) or (Ia) compound of formula or its enantiomer, non-enantiomeric isomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt, wherein the variables are defined in the specification. The invention also relates to the general formula (I) or (Ia) compound of formula or its enantiomer, non-enantiomeric isomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt as the pharmaceutical use, especially as the treatment and prevention of hepatitis b in drug use. (by machine translation)

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A croconium dye, 2,5-bis[(4-carboxylic-piperidylamino)thiophenyl]-croconine (BCTC) based dual signaling probe was found to exhibit colorimetric and fluorescent properties on selective binding towards Fe3+ and Cu2+ in ethanol/water (4:1, v/v) solution, respectively. The binding constants were determined to be 2.12×104 M-1 and 8.58×104 M-1 for Fe3+ and Cu2+, respectively. Most importantly, the 1:1 stoichiometry of the host-guest complexation was confirmed by Job’s method. This result was further confirmed by 1H NMR analysis. Meanwhile, the selectivity experiments revealed that the colorimetric and fluorescent sensor were specific for Fe3+ and Cu2+ even with interference by high concentrations of other metal ions. Moreover, the sensing abilities of the receptor toward Fe3+ and Cu2+ were also investigated by electrochemical technique. The present results indicated that the BCTC chemosensor could be adopted as a selective, sensitive and reversible colorimetric and fluorescent sensor for Fe3+ and Cu2+.

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Background: Natural triterpene boswellic acids (BAs) have attracted much interest due to their anticancer activity, but more chemical modification is necessary to explore their pharmacological value. In addition to subtle functionalization, transformations that alter the triterpene skeleton are viewed as an alternative approach. Objective: In this study, transformations altering ring A of 3-O-acetyl-11-keto-beta-boswellic acid (AKBA) were performed to obtain A-lactone, A-lactam, A-seco and A-contracted derivatives. Method: Thirty-two new derivatives were synthesized, and their structures were confirmed by NMR and MS. Their anticancer activity against human cancer cell lines K562, PC3, A549 and HL60 was screened. Results: Biological evaluation indicated that the ring A cleavage or contraction transformations themselves did not significantly enhance the cytotoxic activity, but most of the derivatives based on these ring A-modified skeletons exhibited good cytotoxic activity. Significantly improved cytotoxicity was discovered for the esterified analogues of the A-lactone and A-lactam series and the amidated analogues of the A-seco and ring A contracted series, especially those bearing two nitrogen-containing substituents. Among them, compounds 6a, 11b, 12k and 18e showed strong cytotoxic activity, with IC50 values of 5.0~3.5 muM against K562 cells, almost ninefold stronger than that of AKBA. Further study proposed that the antiproliferative activities of 6a, 11b, 12k and 18e may be due to apoptosis induction. Conclusion: The transformations of the ring A skeleton of AKBA provide new platforms to discover anticancer candidates.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2971-79-1, molcular formula is C7H13NO2, introducing its new discovery. HPLC of Formula: C7H13NO2

The invention provides compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein Ar1 represents a group (II), (III), (IV) or (V), and A, Ar2, n, R1, R2 , R3, R4 and R5 are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 2971-79-1, name is Methyl piperidine-4-carboxylate, introducing its new discovery. name: Methyl piperidine-4-carboxylate

The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.

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The selective reduction of amides into an intermediate hemiaminal catalyzed by Mo(CO)6 together with the inexpensive and easy to handle TMDS (1,1,3,3-tetramethyldisiloxane) as reducing agent, followed by subsequent trapping of the hemiaminal with a cyanide source, allows for the straightforward synthesis of alpha-amino nitriles. The methodology presented here, displays high levels of chemoselectivity allowing for the reduction of amides in the presence of functional groups such as ketones, imines, aldehydes, and acids, which affords a simple route for the synthesis of alpha-amino nitriles with a broad scope of functionalities in high yields. Furthermore, the applicability of this methodology is demonstrated by scale up experiments and by derivatization of the target compounds into synthetically interesting products. The selective cyanation is successfully applied in late stage functionalizations of amide containing drugs and prolinol derivatives.

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A series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors was developed during our previous work. In the present work, a new series of highly potent bisthiazole-based compounds were designed and synthesized. Among the prepared compounds, compound H13, which contains an alpha-(S)-methyl-substituted benzyl group, displays potent inhibitory activity toward human HDACs and several cancer cells lines. Compound H13 has a favorable PK profile and high tissue distribution specificity in the colon, as well as good efficacy in the AOM-DSS mouse model for colitis-associated colonic tumorigenesis.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2971-79-1, molcular formula is C7H13NO2, introducing its new discovery. Computed Properties of C7H13NO2

The invention relates to novel tricyclic benzazepine derivatives of formula (I), methods for the production thereof, the use thereof for treating and/or preventing diseases, and the use thereof for producing medicaments used for the treatment and/or prophylaxis of diseases, preferably cardiovascular diseases, particularly dyslipidemia, arteriosclerosis, restenosis, and ischemia.

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A one-step rhodium catalyzed direct route from cyclopentadiene (Cpd) to saturated C6-amines is presented via hydroaminomethylation (HAM). The homogeneous catalyst of Rh(ii) octanoate dimer without additional phosphorus ligands was established giving a 77% yield of the monoamine species of Cpd with pyrrolidine within 4 hours. The unwanted reaction of Cpd, the dimerization to dicyclopentadiene (Dcpd), could be suppressed by careful adjustment of the CO : H2 ratio in the synthesis gas and the choice of solvent, both giving the possibility to steer the reaction to selectively produce amines of either Cpd or Dcpd. Furthermore, other investigated cyclic and non-cyclic aliphatic amine substrates showed excellent selectivity up to 100% for the formation of the HAM-products.

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