pubmed-article:18166465 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0027651 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0376358 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0035339 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0334227 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C1512474 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0184511 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0018270 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0520484 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0021469 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C2266853 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C1510480 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0205195 | lld:lifeskim |
pubmed-article:18166465 | lifeskim:mentions | umls-concept:C0217595 | lld:lifeskim |
pubmed-article:18166465 | pubmed:issue | 6 | lld:pubmed |
pubmed-article:18166465 | pubmed:dateCreated | 2008-3-31 | lld:pubmed |
pubmed-article:18166465 | pubmed:abstractText | We have developed new, simple, and efficient procedures for the synthesis of two promising histone deacetylase inhibitors (HDIs), CI-994, (N-(2-aminophenyl)-4-acetylaminobenzamide), and MS-275 (N-(2-aminophenyl)4-[N-(pyridine-3-yl-methoxycarbonyl)aminomethyl]benzamide) from commercially available acetamidobenzoic acid and 3-(hydroxymethyl)pyridine, respectively. The procedures provide CI-994 and MS-275 in 80% and 72% overall yields, respectively. We found that the combination of four HDIs (CI-994, MS-275, SAHA, and TSA) with retinoids all-trans-retinoic acid (ATRA) or 13-cis-retinoic acid (13-CRA) or our atypical retinoic acid metabolism blocking agents (RAMBAs) 1 (VN/14-1) or 2 (VN/66-1) produced synergistic anti-neoplastic activity on human LNCaP prostate cancer cells. The combination of 2 and SAHA induced G1 and G2/M cell cycle arrest and a decrease in the S phase in LNCaP cells. 2+SAHA treatment effectively down-regulated cyclin D1 and cdk4, and up-regulated pro-differentiation markers cytokeratins 8/18 and pro-apoptotic Bad and Bax. Following subcutaneous administration, 2, SAHA or 2+SAHA were well tolerated and caused significant suppression/regression of tumor growth compared with control. These results demonstrate that compound 2 and its combination with SAHA are potentially useful agents that warrant further preclinical development for treatment of prostate cancer. | lld:pubmed |
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pubmed-article:18166465 | pubmed:language | eng | lld:pubmed |
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pubmed-article:18166465 | pubmed:citationSubset | IM | lld:pubmed |
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pubmed-article:18166465 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:18166465 | pubmed:month | Mar | lld:pubmed |
pubmed-article:18166465 | pubmed:issn | 1464-3391 | lld:pubmed |
pubmed-article:18166465 | pubmed:author | pubmed-author:NjarVincent... | lld:pubmed |
pubmed-article:18166465 | pubmed:author | pubmed-author:GediyaLalji... | lld:pubmed |
pubmed-article:18166465 | pubmed:author | pubmed-author:Purushottamac... | lld:pubmed |
pubmed-article:18166465 | pubmed:author | pubmed-author:KhandelwalAak... | lld:pubmed |
pubmed-article:18166465 | pubmed:author | pubmed-author:BelosayAashvi... | lld:pubmed |
pubmed-article:18166465 | pubmed:issnType | Electronic | lld:pubmed |
pubmed-article:18166465 | pubmed:day | 15 | lld:pubmed |
pubmed-article:18166465 | pubmed:volume | 16 | lld:pubmed |
pubmed-article:18166465 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:18166465 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:18166465 | pubmed:pagination | 3352-60 | lld:pubmed |
pubmed-article:18166465 | pubmed:dateRevised | 2009-11-19 | lld:pubmed |
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pubmed-article:18166465 | pubmed:year | 2008 | lld:pubmed |
pubmed-article:18166465 | pubmed:articleTitle | Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts. | lld:pubmed |
pubmed-article:18166465 | pubmed:affiliation | Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201-1559, USA. | lld:pubmed |
pubmed-article:18166465 | pubmed:publicationType | Journal Article | lld:pubmed |