In:
Future Medicinal Chemistry, Future Science Ltd, Vol. 12, No. 15 ( 2020-08), p. 1399-1414
Abstract:
Background: To clarify the molecular mechanism of novel 2-aminonicotinonitrile autophagy enhancers, two series of novel 2-aminonicotinonitrile derivatives are synthesized and their structure–activity relationship and biological activity were analyzed. Results & methodology: Structure–activity relationship analysis revealed that substituents at C-4 and C-6 position of 7a contribute to enhance their autophagy-inducing activity, while C-5 position substituents have the opposite effect. The most promising compound 7g showed the strongest autophagy-inducing activity and better antiproliferative activity by inducing cell apoptosis and blocking cell cycle G1 arrest in SGC-7901 cells. Conclusion: The novel 2-aminonicotinonitrile autophagy enhancers were for the first time discovered and 7g might be a promising new autophagy enhancer with potential anticancer activity.
Type of Medium:
Online Resource
ISSN:
1756-8919
,
1756-8927
DOI:
10.4155/fmc-2019-0244
Language:
English
Publisher:
Future Science Ltd
Publication Date:
2020
SSG:
15,3
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