rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
18
|
pubmed:dateCreated |
2004-8-24
|
pubmed:abstractText |
A series of 9-anilinoacridine N-mustard derivatives, in which the alkylating N-mustard residue was linked to the C-3' or C-4' position of the anilino ring with an O-ethylene spacer, was synthesized and evaluated for cytotoxicity against human lymphoblastic leukemic cells (CCRF-CEM) in culture. The results showed that all of the new compounds exhibited potent cytotoxicity with IC(50) values ranging from 0.002 to 0.7 microM, which were as potent or significantly more potent than 3-(9-acridinylamino)-5-hydroxymethylaniline (AHMA). Compound 9 did not exhibit cross-resistance against both vinblastine-resistant (CCRF-CEM/VBL) and taxol-resistant (CCRF-CEM/taxol) cells. Additionally, compound 9 demonstrated potent antitumor effect in nude mice bearing human breast carcinoma MX-1 xenografts, resulting in complete tumor remission in two out of three mice at the maximal dose of 1-2mg/kg (Q3Dx7) or 3mg/kg (Q4Dx5) via intravenous injection.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Sep
|
pubmed:issn |
0960-894X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
20
|
pubmed:volume |
14
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
4719-22
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:15324894-Amsacrine,
pubmed-meshheading:15324894-Animals,
pubmed-meshheading:15324894-Antineoplastic Agents,
pubmed-meshheading:15324894-Breast Neoplasms,
pubmed-meshheading:15324894-Dose-Response Relationship, Drug,
pubmed-meshheading:15324894-Drug Resistance, Neoplasm,
pubmed-meshheading:15324894-Humans,
pubmed-meshheading:15324894-Injections, Intravenous,
pubmed-meshheading:15324894-Mice,
pubmed-meshheading:15324894-Mice, Nude,
pubmed-meshheading:15324894-Nitrogen Mustard Compounds,
pubmed-meshheading:15324894-Paclitaxel,
pubmed-meshheading:15324894-Structure-Activity Relationship,
pubmed-meshheading:15324894-Tumor Cells, Cultured,
pubmed-meshheading:15324894-Vinblastine,
pubmed-meshheading:15324894-Xenograft Model Antitumor Assays
|
pubmed:year |
2004
|
pubmed:articleTitle |
Potent antitumor N-mustard derivatives of 9-anilinoacridine, synthesis and antitumor evaluation.
|
pubmed:affiliation |
Laboratory of Bioorganic Chemistry, Institute of Biomedical Sciences, Academia Sinica, Taipei 115, Taiwan.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
|