Synthesis and Antiproliferative Activity against Cancer Cells of Indole-Aryl-Amide Derivatives.

ABSTRACT: Indoles constitute a large family of heterocyclic compounds widely occurring in nature which are present in a number of bioactive natural and synthetic compounds, including anticancer agents or atypical opioid agonists. As a result, exponential increases in the development of novel methods for the synthesis of indole-containing compounds have been reported in the literature. A series of indole-aryl amide derivatives 1-7 containing tryptamine or an indolylacetic acid nucleus were designed, synthesized, and evaluated as opioid ligands. These new indole derivatives showed negligible to very low affinity for μ- and δ-opioid receptor (OR). On the other hand, compounds 2, 5 and 7 showed Ki values in the low μM range for κ-OR. Since indoles are well known for th

SUBMITTER: Zhao J 

PROVIDER: S-EPMC9822155 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature