|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
7
|
|
pubmed:dateCreated |
2009-7-6
|
|
pubmed:abstractText |
A new chemical series was identified via high-throughput screening as having antiproliferative activity on DU-145 human prostate carcinoma cell line (hit compound potency - 2.9 microM). Medicinal chemistry optimization of two peripheral diversity vectors of the hit molecule, independently, led to SAR generalizations and identification of the 'best' moieties. The latter were merged in a single compound that exhibited an over 100-fold better potency than the hit compound. For the most potent compounds it was confirmed that the observed antiproliferative potency was not associated with the compounds' non-specific cytotoxicity.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jul
|
|
pubmed:issn |
1521-4184
|
|
pubmed:author |
|
|
pubmed:issnType |
Electronic
|
|
pubmed:volume |
342
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
420-7
|
|
pubmed:meshHeading |
pubmed-meshheading:19544302-Antineoplastic Agents,
pubmed-meshheading:19544302-Cell Death,
pubmed-meshheading:19544302-Cell Line,
pubmed-meshheading:19544302-Cell Line, Tumor,
pubmed-meshheading:19544302-Cell Proliferation,
pubmed-meshheading:19544302-Drug Design,
pubmed-meshheading:19544302-Drug Discovery,
pubmed-meshheading:19544302-Drug Screening Assays, Antitumor,
pubmed-meshheading:19544302-Humans,
pubmed-meshheading:19544302-Male,
pubmed-meshheading:19544302-Nuclear Magnetic Resonance, Biomolecular,
pubmed-meshheading:19544302-Prostatic Neoplasms,
pubmed-meshheading:19544302-Structure-Activity Relationship,
pubmed-meshheading:19544302-Thiazoles
|
|
pubmed:year |
2009
|
|
pubmed:articleTitle |
Discovery and potency optimization of 2-amino-5-arylmethyl-1,3-thiazole derivatives as potential therapeutic agents for prostate cancer.
|
|
pubmed:affiliation |
Department of Lead Discovery, Chemical Diversity Research Institute, Khimki, Moscow Reg., Russia. myk@chemdiv.com
|
|
pubmed:publicationType |
Journal Article
|
