Title

Synthesis And Evaluation Of Unsymmetrical Polyamine Derivatives As Antitumor Agents

Keywords

Antitumor; Cytotoxicity; Synthesis; Unsymmetrical polyamine conjugate

Abstract

A series of unsymmetrically substituted polyamine derivatives were prepared and their cytotoxicities in mouse leukemia L1210, melanoma B16, and HeLa cells were investigated. The in vitro cytotoxicity revealed that these conjugates could recognize the polyamine transporter, and the N-ethyl modified homospermidine moiety may be another efficient carrier as homospermidine even though the introduction of terminal alkyl groups led to reduced cytotoxicity in comparison with the un-substituted counterpart 1. The ornithine decarboxylase and topoisomerase II inhibition experiments indicated that ODC and TOPO II were potential, but not unique targets of these conjugates. Furthermore, the in vivo antitumor activities illustrated that the representative conjugate 2f and the homospermidine analogue 1 evidently inhibited the tumor growth and significantly increased the survival time of mice-bearing sarcoma 180 cells. © 2008 Elsevier Ltd. All rights reserved.

Publication Date

7-15-2008

Publication Title

Bioorganic and Medicinal Chemistry

Volume

16

Issue

14

Number of Pages

7005-7012

Document Type

Article

Personal Identifier

scopus

DOI Link

https://doi.org/10.1016/j.bmc.2008.05.035

Socpus ID

48949115614 (Scopus)

Source API URL

https://api.elsevier.com/content/abstract/scopus_id/48949115614

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