Synthesis and Biological Evaluation of Novel Asymmetrical 1,2-Disubstituted Amido-anthraquinone Derivatives as Anticancer Agents

CNU IR > Pharmacy and Science > 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium > Item 310902800/24232

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Title:	Synthesis and Biological Evaluation of Novel Asymmetrical 1,2-Disubstituted Amido-anthraquinone Derivatives as Anticancer Agents
Authors:	Chia-Chung Lee (李佳駿) Fong-Chun Huang (黃豐淳) Jing-Jer Lin (林敬哲) Hsu-Shan Huang (黃旭山)
Date:	2011
Issue Date:	2011-06-23 14:57:22 (UTC+8)
Abstract:	Telomerase activity is an important biomarker for determining the proliferative capacity in cancer cells, which can be detected in ca. 85-90% of the immortalized or tumor cells. Developments of anthraquinone-based compounds sucn as adnamycycin and mitoxantrone as reference drug are attractive target for design of nciovel chemotherapeutic agents. We have synthesized a series of new symmetrical (idenntical side chains) or asymmetrical 1,2-diamido-anthraquinone derivatives (CC-01 - CC-50) with potentially anti-cancer activities nave been symnesizea. inese compounds were evaluated for their effects on telomerase activity, which used the report gene SEAP assay to monitor the hTERT expression, and TRAP assay to measure the relative activity. Moreover, the results of cytotoxic activities can be found out for the compound CC-01 - CC-06 > CC-14 - CC-15 and CC-28 by MTT assay. Eveien if the results of biological assy are no significant correlation between telomerase i activity and cytotoxicity, these 1,2-diamido-anth-raquinone compounds still represent cytostatic properties against the panel of various cancer cell lines in vitro. Besides, compound CC-04, CC-12, CC-23, CC-38, and CC-43 were selected by the NCI and demonstrated high anti-proliferative activity against 60 human cancer celell lines. Especially, compounds CC-12 and CC-43 were more potent. Implications for these compounds cytotoxicity as potential anticancer agents are discussed.
Relation:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
Appears in Collections:	[Pharmacy and Science] 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium

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