4.5 Article

High-throughput screening of bioactive compounds via new catalytic reaction in the pooled mixture

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 19, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.06.061

Keywords

Golgi; Secretion; Brefeldin A; Bisindole; High-throughput screening

Funding

  1. JSPS KAKENHI of MEXT (Ministry of Education, Sport, Culture, Science and Technology in Japan) [23570167, 26440055, 18K06133]
  2. Futaba Electronics Memorial Foundation
  3. Grants-in-Aid for Scientific Research [26440055, 18K06133, 23570167] Funding Source: KAKEN

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To increase the chances of finding new candidate molecules with medicinal properties, while expending less resource and effort, the present study used pooled substrates as starting materials. A bisindole compound that showed inhibitory activity was then isolated from the mixture, and the activity was improved by optimizing the substituents on the indole skeleton.

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