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A series of 1-arylsulfonyl-5-(N-hydroxyacrylamide)indoles has been identified as a new class of histone deacetylase inhibitors. Compounds 8, 11, 12, 13, and 14 demonstrated stronger antiproliferative activities than 1 (SAHA) with GI50 values ranging from 0.36 to 1.21 muM against Hep3B, MDA-MB-231, PC-3, and A549 human cancer cell lines. Lead compound 8 showed remarkable HDAC 1, 2, and 6 isoenzymes inhibitory activities with IC 50 values of 12.3, 4.0, 1.0 nM, respectively, which are comparable to 1. In in vivo efficacy evaluation against lung A549 xenograft model, 8 displayed better antitumor activity than compound 1.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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A series of 5-(piperidinylethyloxy)quinoline 5-hydroxytryptamine 1D (5-HT1D) receptor antagonists have been discovered from elaboration of the series of dual 5-hydroxytryptamine1-selective serotonin reuptake inhibitors (5HT1-SSRIs) reported previously. This is the first report of highly potent, selective antagonists for the 5-HT 1D receptor, which represents an extremely useful set of pharmacological tools for further understanding the roles of the 5-HT 1 receptor subtypes.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 1074-88-0 is helpful to your research. HPLC of Formula: C9H7NO

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, 1074-88-0, name is 1H-Indole-7-carbaldehyde, introducing its new discovery. HPLC of Formula: C9H7NO

This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: STR1 and their use as LTD4 antagonists.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Eighteen novel chalcone derivatives containing indole and naphthalene moieties (2?19) were synthesized and characterized by 1H-NMR, 13C-NMR and high resolution (HR)-MS spectra. All compounds were evaluated for their in vitro cytotoxic potential against human hepatocellular carcinoma (HepG2), human colon carcinoma (HCT116) and human breast adenocarcinoma (MCF-7) cell lines. Among them, compound 2, 3, 4 and 7 showed potent activities against tested cancer cell lines. More significantly, compound 7 exhibited the most potent cytotoxic activity against HepG2, HCT116 and MCF-7 with IC50 values of 0.65, 1.13 and 0.82muM, respectively. Furthermore, flow cytometry analysis indicated that compound 7 arrested cancer cells in G2/M phase. The compound 7 also displayed significant inhibition of tubulin polymerization (IC50=3.9muM). Finally, molecular docking studies were performed to explore the possible interactions between compound 7 and tubulin binding pockets.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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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, 1074-88-0, name is 1H-Indole-7-carbaldehyde, introducing its new discovery. Application In Synthesis of 1H-Indole-7-carbaldehyde

The reaction of 1-allyl-2-vinyl-1H-pyrroles and 1-allyl-2-vinyl-1H- indoles with arylsilanes in the presence of catalytic [Cp(TMS)2Y(mu-Me)]2 leads to highly selective cyclization/silylation events. In this process the active catalyst for the reaction, ‘Cp(TMS)2YH’, undergoes initial olefin insertion at the vinyl group. Even isopropenyl substituents on the heteroaromatics react in preference to less sterically encumbered allyl groups. Furthermore, the observed regioselectivity reflects an ‘aryl- directed’ process, whereby the more highly substituted secondary or tertiary organometallic is initially generated. This intermediate undergoes cyclization onto the remaining alkene and subsequent silylation by a sigma-bond metathesis reaction, affording the observed products.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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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, 1074-88-0, name is 1H-Indole-7-carbaldehyde, introducing its new discovery. Formula: C9H7NO

Synthesis of a 7-(aminomethyl)indole and related bis-indole derivatives

A 7-(aminomethyl)indole is a useful precursor to form a new range of unsymmetrical and symmetrical 3-substituted amide-, imine-, and amine-linked 7,7?-bis-indoles. The reduction of an imine linked bis-indole leads to formation of the corresponding amine-linked bis-indole.

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Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Gold-catalyzed annulations of 1-(2,3-butadienyl)-1H-indole derivatives

Gold-ringing! Modification of the substitution at C2 drives an entirely different cyclization of N-tethered allenylindoles. An efficient cycloisomerization takes place for the case of R being hydrogen, that is, compatible with additional functional groups. A methyl at C2 precludes this possibility and launches a stepwise process that can be tuned to yield macrocyclic trimers.

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Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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Aminocatalyzed Cascade Synthesis of Enantioenriched 1,7-Annulated Indoles from Indole-7-Carbaldehyde Derivatives and alpha,beta-Unsaturated Aldehydes

We report herein a new cascade strategy for the enantioselective synthesis of 1,7-annulated indoles based on iminium-enamine activation. A careful study of the indole substitution pattern revealed that a chloro substituent at the C-3 position was important to the implementation of the reaction. Employing a diphenylprolinol silyl ether catalyst, a range of 3-chloro-1H-indole-7-carbaldehyde derivatives reacted with alpha,beta-unsaturated aldehydes to afford the corresponding 1,7-annulated indoles in good yields (62-99%) and enantioselectivities (62-92%). Besides the fluorescence properties of the 1,7-ring fused indoles prepared following our methodology, these compounds contain a useful set of functional groups which undergo various synthetic transformations.

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Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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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, 1074-88-0, molcular formula is C9H7NO, introducing its new discovery. HPLC of Formula: C9H7NO

Evaluation of spiropiperidine hydantoins as a novel class of antimalarial agents

Given the rise of parasite resistance to all currently used antimalarial drugs, the identification of novel chemotypes with unique mechanisms of action is of paramount importance. Since Plasmodium expresses a number of aspartic proteases necessary for its survival, we have mined antimalarial datasets for drug-like aspartic protease inhibitors. This effort led to the identification of spiropiperidine hydantoins, bearing similarity to known inhibitors of the human aspartic protease beta-secretase (BACE), as new leads for antimalarial drug discovery. Spiropiperidine hydantoins have a dynamic structure-activity relationship profile with positions identified as being tolerant of a variety of substitution patterns as well as a key piperidine N-benzyl phenol pharmacophore. Lead compounds 4e (CWHM-123) and 12k (CWHM-505) are potent antimalarials with IC50 values against Plasmodium falciparum 3D7 of 0.310 muM and 0.099 muM, respectively, and the former features equivalent potency on the chloroquine-resistant Dd2 strain. Remarkably, these compounds do not inhibit human aspartic proteases BACE, cathepsins D and E, or Plasmodium plasmepsins II and IV despite their similarity to known BACE inhibitors. Although the current leads suffer from poor metabolic stability, they do fit into a drug-like chemical property space and provide a new class of potent antimalarial agents for further study.

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Reference£º
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles