Document Detail

Anticancer activity of a series of platinum complexes integrating demethylcantharidin with isomers of 1,2-diaminocyclohexane.
MedLine Citation:
PMID:  16386904     Owner:  NLM     Status:  MEDLINE    
A series of platinum complexes derived from integrating demethylcantharidin (DMC) with different isomers of 1,2-diaminocyclohexane (DACH) has been synthesized and found to exhibit superior in vitro anticancer activity against colorectal and human hepatocellular cancer cell lines when compared with oxaliplatin, cisplatin, and carboplatin. Flow cytometric analysis revealed that the trans-DACH-Pt-DMC analogues showed similar behavior to oxaliplatin on affecting the cell cycle of the HCT116 colorectal cancer cell line, but distinct from that of cisplatin or carboplatin. The DACH component apparently dictates the trans-DACH-Pt-DMC complexes to behave mechanistically similar to oxaliplatin, whereas the DMC ligand appears to enhance the compounds' overall anticancer activity, probably by accelerating the cell cycle from G1 to S-phase with subsequent onset of G2/M arrest and accompanying apoptosis.
Chun-Wing Yu; Kay K W Li; Siu-Kwong Pang; Steve C F Au-Yeung; Yee-Ping Ho
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-01-04
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  16     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2006 Mar 
Date Detail:
Created Date:  2006-02-07     Completed Date:  2006-04-17     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1686-91     Citation Subset:  IM    
School of Pharmacy, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong SAR, China.
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MeSH Terms
Antineoplastic Agents / chemical synthesis,  chemistry,  pharmacology*
Apoptosis / drug effects
Cantharidin / analogs & derivatives*,  chemistry,  metabolism
Carboplatin / pharmacology
Carcinoma, Hepatocellular / drug therapy
Cell Cycle / drug effects
Cisplatin / pharmacology
Colorectal Neoplasms / drug therapy
Cyclohexylamines / chemistry*,  metabolism
Drug Resistance, Neoplasm
Drug Screening Assays, Antitumor
Flow Cytometry
Liver Neoplasms / drug therapy
Organoplatinum Compounds / pharmacology
Platinum / chemistry*,  metabolism
Tumor Cells, Cultured / drug effects
Reg. No./Substance:
0/Antineoplastic Agents; 0/Cyclohexylamines; 0/Organoplatinum Compounds; 0/demethylcantharidin; 15663-27-1/Cisplatin; 41575-94-4/Carboplatin; 56-25-7/Cantharidin; 63121-00-6/oxaliplatin; 694-83-7/1,2-cyclohexanediamine; 7440-06-4/Platinum

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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