133831-28-4Relevant articles and documents
C3-Formylation of Indoles in Continuous Flow
Sung, Ha Kyoung,Kim, Dong Hyun,Kim, Joon Seok,Park, Chan Pil
supporting information, p. 388 - 392 (2020/12/30)
We have developed a continuous flow C3-formylation technique for indoles using hexamethylenetetramine (HMTA) and iodine. A mixed solvent system of DMF–H2O (1:1, vol/vol) completely dissolves reagents and prevents clogging of microchannels during fluid flow. The continuous flow technique provides maximized mixing and excellent heat transfer efficiency. Thus, flow chemistry accelerates the rate of C3-formylation of indoles in the absence of a strong acid, base, or metal catalyst. We show that high yields of C3-formylated indoles (up to 83%) can be obtained at 150°C when the residence time is as low as 8 min.
2-(1H-INDOLE-3-CARBONYL)-THIAZOLE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS
-
Paragraph 00162; 00394, (2021/06/26)
2-(1H-lndole-3-carbonyl)-thiazole-4-carboxamide derivatives and the corresponding imidazole, oxazole and thiophene derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 27 to 32 and 59 to 219; examples 1 to 8; compounds 1-1 to 1-97; tables 1-a, 2 and 3).
HEPATITIS B CORE PROTEIN MODULATORS
-
Page/Page column 158, (2018/04/13)
The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
MULTIVALENT RAS BINDING COMPOUNDS
-
Paragraph 00727, (2017/07/23)
Described herein are compounds that modulate Ras signaling, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with altered Ras signaling. Further described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds and methods of using such compounds in the treatment of cell proliferative disorders, including cancer.
Synthesis and biological evaluation of indole core-based derivatives with potent antibacterial activity against resistant bacterial pathogens
Hong, Wei,Li, Jingyang,Chang, Zhe,Tan, Xiaoli,Yang, Hao,Ouyang, Yifan,Yang, Yanhui,Kaur, Sargit,Paterson, Ian C,Ngeow, Yun Fong,Wang, Hao
, p. 832 - 844 (2017/07/04)
The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management. To exacerbate this problem, there is currently a serious lack of antibacterial agents that are designed to target extremely drug-resistant bacterial strains. Here we describe the design, synthesis and antibacterial testing of a series of 40 novel indole core derivatives, which are predicated by molecular modeling to be potential glycosyltransferase inhibitors. Twenty of these derivatives were found to show in vitro inhibition of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus. Four of these strains showed additional activity against Gram-negative bacteria, including extended-spectrum beta-lactamase producing Enterobacteriaceae, imipenem-resistant Klebsiella pneumoniae and multidrug-resistant Acinetobacter baumanii, and against Mycobacterium tuberculosis H37Ra. These four compounds are candidates for developing into broad-spectrum anti-infective agents.
Iridium-Catalyzed Direct Regioselective C4-Amidation of Indoles under Mild Conditions
Chen, Shuyou,Feng, Boya,Zheng, Xuesong,Yin, Jiangliang,Yang, Shiping,You, Jingsong
supporting information, p. 2502 - 2505 (2017/05/24)
An efficient Ir-catalyzed amidation of indoles with sulfonyl azides is disclosed, affording diverse C4-amidated indoles exclusively under mild conditions. In this protocol, a variety of indoles with commonly occurring functional groups such as formyl, acetyl, carboxyl, amide, and ester at the C3 position are well tolerated.
Design and Synthesis of 2,2′-Diindolylmethanes to Selectively Target Certain G-Quadruplex DNA Structures
Livendahl, Madeleine,Jamroskovic, Jan,Ivanova, Svetlana,Demirel, Peter,Sabouri, Nasim,Chorell, Erik
, p. 13004 - 13009 (2016/09/09)
G-quadruplex (G4) structures carry vital biological functions, and compounds that selectively target certain G4 structures have both therapeutic potential and value as research tools. Along this line, 2,2′-diindolylmethanes have been designed and synthesi
NBu4NI-catalyzed C3-formylation of indoles with N-methylaniline
Li, Lan-Tao,Huang, Juan,Li, Hong-Ying,Wen, Li-Juan,Wang, Peng,Wang, Bin
supporting information; experimental part, p. 5187 - 5189 (2012/06/01)
nBu4NI-catalyzed C3-selective formylation of N-H and N-substituted indoles by using N-methylaniline as a formylating reagent was first successfully demonstrated.
Mild and selective Ru-catalyzed formylation and Fe-catalyzed acylation of free (N-H) indoles using anilines as the carbonyl source
Wu, Wenliang,Su, Weiping
supporting information; experimental part, p. 11924 - 11927 (2011/09/19)
C3-selective formylation and acylation of free (N-H) indoles under mild conditions can be achieved by using Ru- and Fe-catalyzed oxidative coupling of free (N-H) indoles with anilines, respectively. Both processes are operationally simple, compatible with a variety of functional groups and generally provide the desired products in good yields. 13C-labeling experiments unambiguously established that the carbonylic carbon in the formylation products originated from methyl group of N-methyl aniline.
Method of inhibiting neoplastic cells with indole derivatives
-
, (2008/06/13)
A method for inhibiting neoplasia, particularly cancerous and precancerous lesions, by exposing the affected cells to indole derivatives.
