3,5-Bis(3-alkylaminomethyl-4-hydroxybenzylidene)-4-piperidones: A Novel Class of Potent Tumor-Selective Cytotoxins.
Basic Information
ID: ALA3763040
Journal: J Med Chem
Title: 3,5-Bis(3-alkylaminomethyl-4-hydroxybenzylidene)-4-piperidones: A Novel Class of Potent Tumor-Selective Cytotoxins.
Authors: Karki SS, Das U, Umemura N, Sakagami H, Iwamoto S, Kawase M, Balzarini J, De Clercq E, Dimmock SG, Dimmock JR.
Abstract: Novel 4-piperidone derivatives 2a-f are disclosed as potent cytotoxins. Many of these compounds are more potent than the reference drug melphalan. The compounds in series 2, 4-7 display selective toxicities toward various neoplasms compared to some normal cells. 2a is one of the promising lead molecules that display >11-fold higher growth inhibiting potency than 5-fluorouracil against human colon cancer cells. 2a induces apoptosis, DNA fragmentation, and cleavage of poly ADP-ribose polymerase.
CiteXplore: 26727215
DOI: 10.1021/acs.jmedchem.5b01706
Patent ID: ┄