Document Detail

Synthesis and bioevaluation of N-(arylalkyl)-homospermidine conjugates.
MedLine Citation:
PMID:  17574415     Owner:  NLM     Status:  MEDLINE    
N1-(Arylalkyl)homospermidines (1c-1f) and terminally piperazine-substituted homospermidine conjugates (2a-2e) were synthesized and evaluated for cytotoxicity in mouse leukemia L1210, alpha-difluoromethylornithine (DFMO)-treated L1210, melanoma B16, spermidine (SPD)-treated B16, and HeLa cell lines. Results demonstrated that homospermidine was a more effective vector than piperazine-substituted homospermidine in ferrying diverse arenes into cells via the polyamine transporter. The leading compound, 9-anthracenemethyl-homospermidine (1a), was shown to induce apoptosis in B16 cells and IL-3 dependent FL5.12A pro-B cells. The novel conjugate 4-biphenylmethyl-homospermidine (1e) could also induce apoptosis. However, it exhibited different effect on the cell cycle of B16 cells compared to 1a.
Songqiang Xie; Pengfei Cheng; Guangchao Liu; Yuangfang Ma; Jin Zhao; Mounir Chehtane; Annette R Khaled; Otto Phanstiel; Chaojie Wang
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2007-06-08
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  17     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2007 Aug 
Date Detail:
Created Date:  2007-07-30     Completed Date:  2007-11-21     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  4471-5     Citation Subset:  IM    
Institute of Natural Products & Medicinal Chemistry, Henan University, Henan, Kaifeng 475001, China.
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MeSH Terms
Antineoplastic Agents / chemical synthesis*,  pharmacology*
Apoptosis / drug effects
Cell Line, Tumor
Dose-Response Relationship, Drug
Interleukin-3 / pharmacology
Molecular Structure
Spermidine / analogs & derivatives*,  chemistry*
Structure-Activity Relationship
Reg. No./Substance:
0/Antineoplastic Agents; 0/Interleukin-3; 124-20-9/Spermidine

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