12/10/2022 - Page 8 of 8 - Indole Building Blocks

Wang, Zhen’s team published research in Journal of Medicinal Chemistry in 2019-04-11 | 399-76-8

Journal of Medicinal Chemistry published new progress about Cell migration (inhibited migration and invasiveness of Wnt/β-catenin-dependent cancer cells). 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Application of C9H6FNO2.

Wang, Zhen; Zhang, Min; Wang, Jin; Ji, Haitao published the artcile< Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction>, Application of C9H6FNO2, the main research area is peptidomimetics protein protein interaction inhibitor T Cell Factor.

The β-catenin/T-cell factor (Tcf) protein-protein interaction (PPI) plays a critical role in the β-catenin signaling pathway which is hyperactivated in many cancers and fibroses. Based on compound 1, which was designed to target the Tcf4 G13ANDE17 binding site of β-catenin, extensive structure-activity relationship studies have been conducted. As a result, compounds 53 and 57 were found to disrupt the β-catenin/Tcf PPI with the Ki values of 0.64 and 0.44 μM, resp., and exhibit good selectivity for β-catenin/Tcf over β-catenin/E-cadherin and β-catenin/adenomatous polyposis coli (APC) PPIs. The 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) cell viability assays revealed that 56, the Et ester of 53, was more potent than 53 in inhibiting viability of most of the Wnt/β-catenin hyperactive cancer cells. Further cell-based studies indicated that 56 disrupted the β-catenin/Tcf PPI without affecting the β-catenin/E-cadherin and β-catenin/APC PPIs, suppressed transactivation of Wnt/β-catenin signaling in dose-dependent manners, and inhibited migration and invasiveness of Wnt/β-catenin-dependent cancer cells.

Referemce:
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

Zheng, Ming’s team published research in Organic Letters in 2021-07-02 | 93247-78-0

Organic Letters published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 93247-78-0 belongs to class indole-building-block, and the molecular formula is C10H9NO2, COA of Formula: C10H9NO2.

Zheng, Ming; Hou, Jing; Hua, Li-Li; Tang, Wan-Ying; Zhan, Le-Wu; Li, Bin-Dong published the artcile< Visible-Light-Mediated Divergent Silylfunctionalization of Alkenes>, COA of Formula: C10H9NO2, the main research area is visible light mediated divergent silylfunctionalization alkene hydrosilane; beta alkoxy alkylthio hydroxy indolyl silane preparation.

1,2-Silylfunctionalization of alkenes is an efficient way to construct highly functionalized silicon-containing compounds However, examples of 1,2-silylfunctionalization of alkenes using readily available hydrosilanes are limited. Herein, authors present a visible-light-mediated divergent 1,2-silylfunctionalization of alkenes using hydrosilane under ambient conditions. A series of β-alkoxy, β-alkylthio, β-hydroxy, and β-indolyl silanes was obtained in good to excellent yields. Moreover, vinylsilanes were successfully prepared in the absence of an addnl. nucleophile.

Yang, Ze-ren’s team published research in Chemical Communications (Cambridge, United Kingdom) in 2022 | 93247-78-0

Chemical Communications (Cambridge, United Kingdom) published new progress about Aromatic compounds, azo Role: SPN (Synthetic Preparation), PREP (Preparation). 93247-78-0 belongs to class indole-building-block, and the molecular formula is C10H9NO2, Name: Methyl 1H-indole-7-carboxylate.

Yang, Ze-ren; Zhang, Bo; Long, Yong-jie; Shi, Min published the artcile< Palladium-catalyzed hydroamination of vinylidenecyclopropane-diester with pyrroles and indoles: an approach to azaaromatic vinylcyclopropanes>, Name: Methyl 1H-indole-7-carboxylate, the main research area is indole vinylidienecyclopropane diester palladium catalyst hydroamination; dialkyl vinylcyclopropane dicarboxylate indole preparation; pyrrole vinylidienecyclopropane diester palladium catalyst hydroamination; diethyl vinylcyclopropane dicarboxylate pyrrole preparation.

A new method for the synthesis of azaarom. vinylcyclopropanes (VCPs) was disclosed in this paper by using pyrrole or indole derivatives as nucleophilic reagents to react with vinylidenecyclopropane-diesters (VDCP-diesters) in the presence of a Pd catalyst, a phosphine ligand and a base under mild conditions in up to 98% yield with a reasonable substrate scope. This reaction was one of the few examples of hydroamination at electron-rich allene’s β-position. A plausible reaction mechanism has also been proposed through a zwitterionic π-propargyl N-palladium species according to the previous work and the obtained deuterium labeling exptl. result.

Cengiz, Nergiz’s team published research in Macromolecular Chemistry and Physics in 2019 | 950846-89-6

Macromolecular Chemistry and Physics published new progress about Cations. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Safety of 2-(2-Aminoethyl)-3′,6′-bis(diethylamino)spiro[isoindoline-1,9′-xanthen]-3-one.

Cengiz, Nergiz published the artcile< Fabrication of Multifunctional Stimuli-Responsive Hydrogels Susceptible to both pH and Metal Cation for Visual Detections>, Safety of 2-(2-Aminoethyl)-3′,6′-bis(diethylamino)spiro[isoindoline-1,9′-xanthen]-3-one, the main research area is multifunctional stimuli responsive hydrogel pH metal cation colorimetric sensor.

Advances in several areas of contemporary biomaterial science are closely related to the design of stimuli-responsive smart materials. An important aspect that governs widespread adaptation of a synthetic biomaterial depends on its ease of synthesis, as well as facile functionalization. Readily available homo-bifunctional PEG-based diamines are mixed with a tetra-arm epoxide based cross-linker to yield hydrogels through the epoxy-amine addition reaction. Hydrogels obtained with varying chain lengths of PEG polymer were characterized for their morphol., swelling, and rheol. properties. The residual epoxide groups within the hydrogel were used for post-gelation functionalization to obtain a functional material. In particular, functionalization with an amine-containing rhodamine derivative yields a hydrogel that serves as a colorimetric sensor for acidic pH environment, and indicates Fe3+ cation with high specificity.