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Synthesis, Characterization, and Molecular Docking Studies of N-Acylated Butyro and Valerolactam Derivatives with Antiproliferative and Cytotoxic Activities

Quimque, Mark Tristan J. ; Mandigma, Mark John P. ; Lim, Justin Allen K. ; Budde, Simon ; Dahse, Hans-Martin ; Villaflores, Oliver B. ; Hallare, Arnold V. ; Macabeo, Allan Patrick G.



Abstract

Background: Electrophilic compounds bearing Michael acceptors present great promise in anticancer drug discovery. Methods: Drawing inspirations from cytotoxic Piper lactam alkaloids, twelve N-acylated butyro- and valerolactams were prepared and evaluated for antiproliferative and cytotoxic activities against the normal human umbilical vein endothelial cells (HUVEC), chronic human myeloid leukemia ...

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