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We report structure-activity relationships of 1-arylsulfonyl indoline based benzamides. The benzamide (9) exhibits striking tubulin inhibition with an IC50 value of 1.1 muM, better than that of combretastain A-4 (3), and substantial antiproliferative activity against a variety of cancer cells, including MDR-positive cell lines with an IC50 value of 49 nM (KB), 79 nM (A549), 63 nM (MKN45), 64 nM (KB-VIN10), 43 nM (KB-S15), and 46 nM (KB-7D). Dual inhibitory potential of compound 9 was found as it demonstrated significant inhibitory potential against HDAC1, 2 and 6 in comparison to MS-275 (6). Some key interactions of 9 with the amino acid residues of the active site of tubulin and with amino acid residues of HDAC 1 isoform have been figured out by molecular modeling. Compound 9 also demonstrated significant in vivo efficacy in the human non-small cell lung cancer A549 xenograft model as well as B-cell lymphoma BJAB xenograft tumor model.

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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

Electric Literature of 1074-88-0, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.1074-88-0, Name is 1H-Indole-7-carbaldehyde, molecular formula is C9H7NO. In a article，once mentioned of 1074-88-0

The EP3 receptor on the platelet mediates prostaglandin E 2 potentiation of thrombogenic coagonists including collagen and adenosine diphosphate (ADP). A pharmacophore driven approach led to the identification of diverse peri-substituted heterocycles as potent and selective EP3 receptor antagonists. A simultaneous chemical optimization and druglike assessment of prioritized molecules converged on a lead compound 50 (DG-041) that displayed favorable in vitro and functional activities as an inhibitor of human platelet aggregation. This agent is currently in human clinical trials for the treatment of atherothrombosis.

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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

Reference of 1074-88-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1074-88-0, Name is 1H-Indole-7-carbaldehyde, molecular formula is C9H7NO. In a Article，once mentioned of 1074-88-0

Transient intermediates as highly reactive species are difficult to manipulate due to their poor stability. Stabilization of unstable intermediates for functionalization is an attractive approach, but the practical applications are still rare. Herein, we explore a strategy that could effectively stabilize labile 3-chloroindolenines and significantly improve the lifetime from seconds to weeks. This chemistry was utilized to enable the synthesis of 55 diverse compounds which are unable to be achieved by traditional approach.

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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

Reference of 1074-88-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1074-88-0, Name is 1H-Indole-7-carbaldehyde, molecular formula is C9H7NO. In a Article，once mentioned of 1074-88-0

3-Acyl-indole derivative 1 was identified as a novel dengue virus (DENV) inhibitor from a DENV serotype 2 (DENV-2) phenotypic antiviral screen. Extensive SAR studies led to the discovery of new derivatives with improved DENV-2 potency as well as activity in nanomolar to micromolar range against the other DENV serotypes. In addition to the potency, physicochemical properties and metabolic stability in rat and human microsomes were improved during the optimization process. Chiral separation of the racemic mixtures showed a clear preference for one of the two enantiomers. Furthermore, rat pharmacokinetics of two compounds will be discussed in more detail, demonstrating the potential of this new series of pan-serotype-DENV inhibitors.

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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

Electric Literature of 1074-88-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1074-88-0, Name is 1H-Indole-7-carbaldehyde, molecular formula is C9H7NO. In a Article，once mentioned of 1074-88-0

A series of N-substituted (2-phenylcyclopropyl)methylamines were designed and synthesized, with the aim of finding serotonin 2C (5-HT2C)-selective agonists with a preference for Gq signaling. A number of these compounds exhibit 5-HT2C selectivity with a preference for Gq-mediated signaling compared with beta-arrestin recruitment. Furthermore, the N-methyl compound (+)-15a, which displayed an EC50 of 23 nM in the calcium flux assay while showing no beta-arrestin recruitment activity, is the most functionally selective 5-HT2C agonist reported to date. The N-benzyl compound (+)-19, which showed an EC50 of 24 nM at the 5-HT2C receptor, is fully selective over the 5-HT2B receptor. In an amphetamine-induced hyperactivity model, compound (+)-19 showed significant antipsychotic-drug-like activity. These novel compounds shed light on the role of functional selectivity at the 5-HT2C receptor with respect to antipsychotic activity.

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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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Excited state intramolecular proton transfer (ESIPT) has been studied in Indole-7-Carboxaldehyde (I7C). DFT, TDDFT, CIS theories with B3LYP/6-311++G (d, p), etc. basis sets have been used to obtain structural parameters and energies of I7C in ground, excited states for cis (Nc), trans (Nt) and zwitterionic (Z) conformers. Photo-physical pathway involving ESIPT from cis (Nc) to zwitterion (Z) agrees well with the dual fluorescence at 451 and 862 nm obtained from computed results and experimental observations. Potential energy surface scan confirms the existence of ESIPT by asymmetric double minima in the excited state pathway along the Reaction Coordinate -N 15-H12 donor.

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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

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Application In Synthesis of 1H-Indole-7-carbaldehyde, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1074-88-0, Name is 1H-Indole-7-carbaldehyde, molecular formula is C9H7NO. In a Patent, authors is ，once mentioned of 1074-88-0

Disclosed are novel reverse turn mimetics based on the framework of pyrazino-triazinone, and the use thereof in the treatment of cancers, particularly, acute myeloid leukemia. A method is also provided for manufacturing the reverse turn mimetics on a mass scale.

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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

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent， Recommanded Product: 1074-88-0, Which mentioned a new discovery about 1074-88-0

A new series of gallic hydrazones containing an indole moiety was synthesized through the reaction of gallic hydrazide and different indole carboxaldehydes. Their antioxidant activities were determined on DPPH radical scavenging and inhibition of lipid peroxidation. The in-vitro cytotoxic activities of the compounds were evaluated against HCT-116 (human colon cancer cell line) and MCF-7 (estrogen-dependent human breast cancer cell line) by the MTT method. An attempt to correlate the biological results with their structural characteristics has been done. A limited positive structure activity relationship was found between cytotoxic and antioxidant activities. Gallic acid derivatives are naturally occurring compounds with interesting biological properties. Similarly, indolic compounds represent an important class of therapeutical agents in medicinal chemistry. A series of hybrid molecules incorporating these two pharmacophores has been synthesized and assessed for their antioxidant and cytotoxic activities. Copyright

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, Recommanded Product: 1074-88-0, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 1074-88-0

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

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Quality Control of: 1H-Indole-7-carbaldehyde, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1074-88-0, Name is 1H-Indole-7-carbaldehyde, molecular formula is C9H7NO. In a Article, authors is Al-awar, Rima S.，once mentioned of 1074-88-0

The synthesis of novel aza-1,7-annulated indoles was achieved and these were converted to indolocarbazoles that proved to be potent kinase inhibitors. These compounds were also evaluated in a human colon carcinoma cell line and proved to be good antiproliferative agents.

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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

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Safety of 1H-Indole-7-carbaldehyde, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1074-88-0, Name is 1H-Indole-7-carbaldehyde, molecular formula is C9H7NO. In a Article, authors is Lai, Mei-Jung，once mentioned of 1074-88-0

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