Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives: Their cytoprotection effect from rotenone toxicity and preliminary DMPK properties期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives: Their cytoprotection effect from rotenone toxicity and preliminary DMPK properties

Authors:	Yuefen Zhou Gang Liu Jinhua Chen P.S. Murali Mohan Reddy Il Sang Yoon Menghua Zhang Bin Zhang Jack R. Barber Shi Chung Ng

Affiliation:	CytRx Corporation, 3030 Bunker Hill Street, Suite 101, San Diego, CA 92109, USA

Abstract:	Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives exhibited potent cytoprotective effect from rotenone toxicity. Lead optimization focused on the CC₅₀/EC₅₀ ratio and DMPK properties led to the overall improvement of the compound profile of this series with high CC₅₀/EC₅₀ ratio (92 for 1f), good metabolic stability in rat microsomes and medium to high aqueous solubility.

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