910488-04-9Relevant academic research and scientific papers
TYLOPHORINE ANALOGS AS ANTITUMOR AGENTS
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Page/Page column 28-29, (2008/06/13)
Compounds of Formula I are described: preferably subject to the proviso that either (a) R2 and R3 together form -O-CH(R10)-O-, or (b) R5 and R6 together form -O-CH(R10)-O-, wherein R10
Antitumor agents 251: Synthesis, cytotoxic evaluation, and structure-activity relationship studies of phenanthrene-based tylophorine derivatives (PBTs) as a new class of antitumor agents
Wei, Linyi,Brossi, Arnold,Kendall, Ross,Bastow, Kenneth F.,Morris-Natschke, Susan L.,Shi, Qian,Lee, Kuo-Hsiung
, p. 6560 - 6569 (2007/10/03)
Polar phenanthrene-based tylophorine derivatives (PBTs) were designed, synthesized and evaluated as potential antitumor agents. These compounds contain a core phenanthrene structure and can be synthesized efficiently in excellent yield. The newly synthesized PBTs were evaluated for cytotoxic activity against the A549 human cancer cell line. Among them, N-(2,3-methylenedioxy-6-methoxy-phenanthr-9-ylmethyl)-l-2-piperidinemethanol (34) and N-(2,3-methylenedioxy-6-methoxy-phenanthr-9-ylmethyl)-5-aminopentanol (28) showed the highest potency with IC50 values of 0.16 and 0.27 μM, respectively, which are comparable to those of currently used antitumor drugs. A structure-activity relationship (SAR) study was also explored to facilitate the further development of this new compound class.
