N-Polybenzylated alicyclic 1,2-diamines: cytotoxicity and G1 phase arrest in cancer cell line

Antonio Caldarelli; Valeria De Biasio; Giovanni B Giovenzana; Gianpiero Mastronardo; Roberto Negri

doi:10.1007/s11030-014-9519-5

N-Polybenzylated alicyclic 1,2-diamines: cytotoxicity and G1 phase arrest in cancer cell line

Mol Divers. 2014 Nov;18(4):879-86. doi: 10.1007/s11030-014-9519-5. Epub 2014 Jun 28.

Authors

Antonio Caldarelli¹, Valeria De Biasio, Giovanni B Giovenzana, Gianpiero Mastronardo, Roberto Negri

Affiliation

¹ Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale "A. Avogadro", L.go Donegani 2, I-28100 , Novara NO, Italy.

PMID: 24973276
DOI: 10.1007/s11030-014-9519-5

Abstract

Cytotoxicity in the μM range was observed in cancer cell lines treated with N,N,N',N'-tetrabenzyl-4,5-diamino-2-cyclopentenone. Cell cycle analysis on HeLa cells showed a clear G1 phase arrest. A preliminary SAR on structural analogs was performed in order to identify the pharmacophores.

MeSH terms

Antineoplastic Agents / pharmacology*
Antineoplastic Agents / toxicity
Cell Line, Tumor
Cell Survival / drug effects
Diamines / chemical synthesis
Diamines / pharmacology*
Diamines / toxicity
Dose-Response Relationship, Drug
G1 Phase Cell Cycle Checkpoints / drug effects*
Humans

Substances

Antineoplastic Agents
Diamines