910488-32-3Relevant academic research and scientific papers
Antitumor agents 253. Design, synthesis, and antitumor evaluation of novel 9-substituted phenanthrene-based tylophorine derivatives as potential anticancer agents
Wei, Linyi,Shi, Qian,Bastow, Kenneth F.,Brossi, Arnold,Morris-Natschke, Susan L.,Nakagawa-Goto, Kyoko,Wu, Tian-Shung,Pan, Shiow-Lin,Teng, Che-Ming,Lee, Kuo-Hsiung
, p. 3674 - 3680 (2007)
C9-Substituted phenanthrene-based tylophorine derivatives (PBTs) (13-36) were synthesized and evaluated as in vitro anticancer agents against the human A549 lung cancer cell line. Twelve active compounds were further examined against DU-145 (prostate), ZR-751 (breast), KB (nasopharyngeal), and KB-Vin (multidrug resistant KB subline) human cancer cell lines. They showed potent cytotoxic activity against both wild type and matched multidrug resistant KB cell lines, and displayed notable selectivity toward DU-145 (prostate) and ZR-751 (breast) cancer cell lines. The mode of action of this class may be distinctly different from that of other cancer chemotherapeutic compounds. Three PBT analogs were also evaluated in a murine model. Compound 24b showed modest in vivo antitumor activity against human A549 xenograft in nude mice as well as potent in vitro cytotoxic activity, and thus, is a promising anticancer lead compound.
TYLOPHORINE ANALOGS AS ANTITUMOR AGENTS
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Page/Page column 25, (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.
