Synthesis of Polycyclic Indolines via Spiroindolenines: Mechanistic Validation and HDAC6 Inhibition Potential
Bo-Bo Gou1, Chao-Feng Chong1, Zhi-Yong Lu2
1Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education, College of Chemistry & Materials Science, Northwest University, Xi'an 710127, P. R. China.
Abstract:
A highly selective and acid-controlled method for the synthesis of functionalized pentacyclic indolines from tryptophols and o-aminobenzaldehydes is described. Preliminary mechanistic studies provide direct evidence of the involvement of a spiroindolenine intermediate. Furthermore, computational evaluation reveals the products' strong binding affinity and conformational stability against HDAC6, suggesting their attractive pharmacological profile as promising lead candidates worthy of further investigation.
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