59496-25-2Relevant academic research and scientific papers
A flexible, convergent approach to polycyclic indole structures: Formal synthesis of (±)-mersicarpine
Blechy, Aurellen,Zard, Samir Z.
, p. 2800 - 2803 (2009)
The formal synthesis of (±)-mersicarpine was achieved using an lntermolecular radical addition-radical cyclization cascade. This key reaction represents a flexible, convergent route to numerous polycyclic indole derivatives.
Structure revision of the rare sponge metabolite echinosulfone A, and biosynthetically related echinosulfonic acids A–D
Neupane, Pratik,Salim, Angela A.,Capon, Robert J.
, (2020)
A short Friedel-Crafts mediated total synthesis has informed structure revision of the rare marine sponge natural product echinosulfone A (1a) and the biosynthetically related echinosulfonic acids A–D (2a–5a).
Synthesis and Pharmacological Profiling of the Metabolites of Synthetic Cannabinoid Drugs APICA, STS-135, ADB-PINACA, and 5F-ADB-PINACA
Longworth, Mitchell,Connor, Mark,Banister, Samuel D.,Kassiou, Michael
, p. 1673 - 1680 (2017)
Synthetic cannabinoids (SCs) containing a 1-pentyl-1-H substituted indole or indazole are abused around the world and are associated with an array of serious side effects. These compounds undergo extensive phase 1 metabolism after ingestion with little understanding whether these metabolites are contributing to the cannabimimetic activity of the drugs. This work presents the synthesis and pharmacological characterization of the major metabolites of two high concern SCs; APICA and ADB-PINACA. In a fluorometric assay of membrane potential, all metabolites that did not contain a carboxylic acid functionality retained potent activity at both the CB1 (EC50 = 14-787 nM) and CB2 (EC50 = 5.5-291 nM) receptors regardless of heterocyclic core or 3-carboxamide substituent. Of note were the 5-hydroxypentyl and 4-pentanone metabolites which showed significant increases in CB2 functional selectivity. These results suggest that the metabolites of SCs potentially contribute to the overall pharmacological profile of these drugs.
Palladium-Catalyzed Silacyclization of (Hetero)Arenes with a Tetrasilane Reagent through Twofold C?H Activation
Wang, Dingyi,Li, Mingjie,Chen, Xiangyang,Wang, Minyan,Liang, Yong,Zhao, Yue,Houk, Kendall N.,Shi, Zhuangzhi
supporting information, p. 7066 - 7071 (2021/03/01)
The use of an operationally convenient and stable silicon reagent (octamethyl-1,4-dioxacyclohexasilane, ODCS) for the selective silacyclization of (hetero)arenes via twofold C?H activation is reported. This method is compatible with N-containing heteroarenes such as indoles and carbazoles of varying complexity. The ODCS reagent can also be utilized for silacyclization of other types of substrates, including tertiary phosphines and aryl halides. A series of mechanistic experiments and density functional theory (DFT) calculations were used to investigate the preferred pathway for this twofold C?H activation process.
PYRIMIDINE COMPOUND, PREPARATION METHOD THEREOF AND MEDICAL USE THEREOF
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Paragraph 0359; 0362; 0363, (2021/04/10)
The present invention discloses a pyrimidine compound, a preparation method thereof and a medical use thereof. Specifically, the present invention discloses a pyrimidine compound represented by formula (I), pharmaceutically acceptable salts thereof, a preparation method thereof, and a use thereof as a cyclin-dependent kinase 9 (CDK9) inhibitor, particularly for the treatment of cancer. The definition of each group in formula (I) is the same as that in the specification.
Indole derivative as well as preparation method and application thereof
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Paragraph 0063-0065, (2021/06/23)
The invention discloses an indole derivative as well as a preparation method and application thereof, belongs to the technical field of medicines, and particularly relates to an indole derivative as shown in a general formula I, the invention also relates
Compound capable of inhibiting activity of organic anion transporter 1 as well as preparation method and application of compound
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Paragraph 0052-0054; 0059-0061; 0174-0176, (2021/06/23)
The invention discloses a compound capable of inhibiting the activity of an organic anion transporter 1 as well as a preparation method and application of the compound, belongs to the technical field of medicines, and provides a compound which has a brand-new structure and is shown in a general formula I and has the activity of inhibiting the organic anion transporter 1. The invention also provides a preparation method of the compound and application of the compound in medicines for treating and/or preventing hyperuricemia and gout diseases. A new product is provided for developing a novel organic anion transporter 1 inhibitor, a new treatment thought is provided for treating hyperuricemia and gout, meanwhile, a preparation method is provided for preparing the compound, and certain guiding significance is achieved.
Preparation method of tropisetron hydrochloride
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Paragraph 0016, (2020/03/09)
The invention discloses a preparation method of tropisetron hydrochloride (I). According to the preparation method, an amide solvent is used as a solvent, and chlorination and esterification are performed to obtain tropisetron hydrochloride. The preparation method disclosed by the invention is low in cost and simple and convenient to operate, can be used for large-scale production, and lays a solid foundation for quality research on bulk drugs and related preparations of tropisetron hydrochloride.
Design, synthesis, and evaluation of novel anti-trypanosomal compounds
Lepovitz, Lance T.,Martin, Stephen F.,Meis, Alan R.,Mensa-Wilmot, Kojo,Pham, Alexandra,Thomas, Sarah M.,Wiedeman, Justin
supporting information, (2020/03/25)
Human African trypanosomiasis (HAT) is a deadly neglected tropical disease caused by the protozoan parasite Trypanosoma brucei. During the course of screening a collection of diverse nitrogenous heterocycles, we discovered two novel compounds that contain the tetracyclic core of the Yohimbine and Corynanthe alkaloids, were potent inhibitors of T. brucei proliferation and T. brucei methionyl-tRNA synthetase (TbMetRS) activity. Inspired by these key findings, we prepared several novel series of hydroxyalkyl δ-lactam, δ-lactam, and piperidine analogs and tested their anti-trypanosomal activity. A number of inhibitors were more potent against T. brucei than these initial hits with one hydroxyalkyl δ-lactam derivative being 25-fold more effective in our assay. Surprisingly, most of these active compounds failed to inhibit TbMetRS. This work underscores the importance of verifying, irrespective of close structural similarities, that new compounds designed from a lead with a known biological target engage the putative binding site.
METHODS OF TREATING CANCER
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Paragraph 00215-00216; 00505, (2020/06/10)
The present disclosure relates to methods of treating cancer in a patient using a combination of an inhibitor of an immune checkpoint protein and an indole compound or its phosphate derivative.
