- Synthesis and biological evaluation of tylophorine-derived dibenzoquinolines as orally active agents: Exploration of the role of tylophorine e ring on biological activity
-
A series of novel tylophorine-derived dibenzoquinolines has been synthesized and their biological activity evaluated. Three assays were conducted: inhibition of cancer cell proliferation, inhibition of TGEV replication for anticoronavirus activity, and su
- Lee, Yue-Zhi,Yang, Cheng-Wei,Hsu, Hsing-Yu,Qiu, Ya-Qi,Yeh, Teng-Kuang,Chang, Hsin-Yu,Chao, Yu-Sheng,Lee, Shiow-Ju
-
p. 10363 - 10377
(2013/02/22)
-
- When inhibitors do not inhibit: Critical evaluation of rational drug design targeting chorismate mutase from mycobacterium tuberculosis
-
Tuberculosis (TB) is a devastating disease that claims millions of lives every year. Hindered access or non-compliance to medication, especially in developing countries, led to drug resistance, further aggravating the situation. With current standard ther
- Munack, Steffi,Leroux, Vincent,Roderer, Kathrin,?kvist, Mats,Van Eerde, André,Gundersen, Lise-Lotte,Krengel, Ute,Kast, Peter
-
p. 2507 - 2527
(2013/01/16)
-
- Antitumor agents 251: Synthesis, cytotoxic evaluation, and structure-activity relationship studies of phenanthrene-based tylophorine derivatives (PBTs) as a new class of antitumor agents
-
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.
- Wei, Linyi,Brossi, Arnold,Kendall, Ross,Bastow, Kenneth F.,Morris-Natschke, Susan L.,Shi, Qian,Lee, Kuo-Hsiung
-
p. 6560 - 6569
(2007/10/03)
-
- Intramolecular amidation - An efficient synthesis of 3-aryl-2-quinolinones
-
To reveal the scope of the syntheses of 3-aryl-2-quinolinones from 2-nitro-α-phenylcinnamic acids, the isomerization of (E)-2-amino-α- phenylcinnamic acids was studied. The results showed that (E)-2-amino-α- phenylcinnamic acids were isomerized to its (Z)
- Luo, Yinggang,Tao, Feiyan,Liu, Yan,Li, Bogang,Zhang, Guolin
-
p. 1620 - 1625
(2007/10/03)
-
- Total syntheses of (±)-cryptopleurine, (±)-antofine and (±)- deoxypergularinine
-
The alkaloids (±)-cryptopleurine 1, (±)-antofine 2, and (±)- deoxypergularinine 3 were synthesized by Pictet-Spengler cyclization of the 2-arylmethylpiperidine and -pyrrolidines 4, 5 and 6 obtained by sequential N- deprotection-reduction of the parent ene
- Lebrun, Stephane,Couture, Axel,Deniau, Eric,Grandclaudon, Pierre
-
p. 2659 - 2670
(2007/10/03)
-