ArticleACS medicinal chemistry letters2016
Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 52 citations in OpenAlex.
- Green Light Promoted Iridium(III)/Copper(I)-Catalyzed Addition of Alkynes to Aziridinoquinoxalines Through the Intermediacy of Azomethine Ylides.Angewandte Chemie (International ed. in English) · 2024Article
- Rhodium-Catalyzed Asymmetric Functionalization of Quinoxalinium Salts.Organic letters · 2023Article
- Development and Application of Indolines in Pharmaceuticals.ChemistryOpen · 2023Review
- Selective Iron Catalyzed Synthesis of N-Alkylated Indolines and Indoles.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Controllable access to trifluoromethyl-containing indoles and indolines: palladium-catalyzed regioselective functionalization of unactivated alkenes with trifluoroacetimidoyl chlorides.Chemical science · 2022Article
- Catalytic asymmetric synthesis ofChemical science · 2021Article
- Anti-selective [3+2] (Hetero)annulation of non-conjugated alkenes via directed nucleopalladation.Nature communications · 2020Article
- The role of NMR in leveraging dynamics and entropy in drug design.Journal of biomolecular NMR · 2020Article
- Photocatalytic enantioselective α-aminoalkylation of acyclic imine derivatives by a chiral copper catalyst.Nature communications · 2019Article
- Intramolecular radical cyclization approach to access highly substituted indolines and 2,3-dihydrobenzofurans under visible-light.RSC advances · 2018Article
- Literature Survey and Further Studies on the 3-Alkylation of N-Unprotected 3-Monosubstituted Oxindoles. Practical Synthesis of N-Unprotected 3,3-Disubstituted Oxindoles and Subsequent Transformations on the Aromatic Ring.Molecules (Basel, Switzerland) · 2016Review
Corrections and comments
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Authors and funding
17 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Using the collective body of known (CETP) inhibitors as inspiration for design, a structurally novel series of tetrahydroquinoxaline CETP inhibitors were discovered. An exemplar from this series, compound 5, displayed potent in vitro CETP inhibition and was efficacious in a transgenic cynomologus-CETP mouse HDL PD (pharmacodynamic) assay. However, an undesirable metabolic profile and chemical instability hampered further development of the series. A three-dimensional structure of tetrahydroquinoxaline inhibitor 6 was proposed from (1)H NMR structural studies, and this model was then used in silico for the design of a new class of compounds based upon an indoline scaffold. This work resulted in the discovery of compound 7, which displayed potent in vitro CETP inhibition, a favorable PK-PD profile relative to tetrahydroquinoxaline 5, and dose-dependent efficacy in the transgenic cynomologus-CETP mouse HDL PD assay.
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