3,5-Bis(benzylidene)-1-[3-(2-hydroxyethylthio)propanoyl]piperidin-4-ones: A Novel Cluster of Potent Tumor-Selective Cytotoxins — Umashankar Das (2011) | RDL Network
3,5-Bis(benzylidene)-1-[3-(2-hydroxyethylthio)propanoyl]piperidin-4-ones: A Novel Cluster of Potent Tumor-Selective Cytotoxins
Article 2011 en
Authors
UD
Umashankar Das
HP
Hari N. Pati
HS
Hiroshi Sakagami
Abstract
1 min read
Novel 3,5-bis(benzylidene)-1-[3-(2-hydroxyethylthio)propanoyl]piperidin-4-ones (3a-e) display potent cytotoxicity and a preferential lethality toward various neoplasms compared to some normal cells. The corresponding sulfonic acid analogues 5a-e and an isostere 4 demonstrated substantially lower activity. The leads 3d and 3e possess very high activity against colon cancer and leukemia cell lines, caused DNA fragmentation, and activated caspase-3 in HL-60 cells. The enones 3b-e were well tolerated in a short-term toxicity screen in mice.
Swagatika Das, Umashankar Das, Armando Varela‐Ramírez, Carolina Lema, Renato J. Aguilera, Jan Balzarini, De Clercq Erik, Stephen G. Dimmock, Dennis K.J. Gorecki, Jonathan R. Dimmock
Swagatika Das, Umashankar Das, Ponniah Selvakumar, Rajendra K. Sharma, Jan Balzarini, De Clercq Erik, Joséph Molnár, Julianna Serly, Zoltán Baráth, G. Schatte, Brian Bandy, Dennis K.J. Gorecki, Jonathan R. Dimmock
Subhas S. Karki, Umashankar Das, Naoki Umemura, Hiroshi Sakagami, Shoko Iwamoto, Masami Kawase, Jan Balzarini, De Clercq Erik, Stephen G. Dimmock, Jonathan R. Dimmock
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