- Design, synthesis, biological evaluation and molecular modeling study of novel macrocyclic bisbibenzyl analogues as antitubulin agents
-
A series of macrocyclic bisbibenzyls with novel skeletons was designed, synthesized, and evaluated for antiproliferative activity against five anthropic cancer cell lines. Among these novel molecules, compound 47 displayed excellent anticancer activity ag
- Sun, Bin,Li, Lin,Hu, Qing-wen,Zheng, Hong-bo,Tang, Hui,Niu, Huan-min,Yuan, Hui-qing,Lou, Hong-xiang
-
p. 186 - 208
(2017/02/26)
-
- Design, synthesis and biological evaluation of novel macrocyclic bisbibenzyl analogues as tubulin polymerization inhibitors
-
A series of novel macrocyclic bisbibenzyl analogues was designed, synthesized, and evaluated for their antiproliferative activity in vitro. All of the compounds were tested in five anthropic cancer cell lines, including a multidrug-resistant phenotype. Among these novel molecules, compounds 88, 92 and 94 displayed excellent anticancer activity against Hela, k562, HCC1428, HT29, and PC-3/Doc cell lines, with average IC50 values ranging from 2.23 μM to 3.86 μM, and were more potent than the parental compound marchantin C and much more potent than the positive control Adriamycin. In addition, the mechanism of action of compound 88 was investigated by cell cycle analysis and a tubulin polymerization assay in HCC1482 cells. The binding mode of compound 88 to tubulin was also investigated utilizing a molecular docking study. In conclusion, the present study improves our understanding of the action of bisbibenzylbased tubulin polymerization inhibitors and provides a new molecular scaffold for the further development of antitumor agents that target tubulin.
- Sun, Bin,Li, Lin,Hu, Qing-Wen,Xie, Fei,Zheng, Hong-Bo,Niu, Huan-Min,Yuan, Hui-Qing,Lou, Hong-Xiang
-
p. 484 - 499
(2016/07/06)
-
- Alkylations of chiral imidazolidinones derived from di- and triglycine and attempts at cyclisations to give cycloisodityrosines
-
Di- and triglycine derivatives (1-5) containing a 2-tert-butyl-1,3-imidazolidin-4-one moiety were prepared in rac. and enantiopure forms. By deprotonations with LiNR2 these imidazolidinones were converted to Li, Li2, and Li3/su
- Bezencon, Olivier,Seebach, Dieter
-
p. 1259 - 1276
(2007/10/03)
-
- Total Syntheses of Riccardins A, B, and C, Cytotoxic Macrocyclic Bis(bibenzyls) from Liverworts
-
Di-O-methylriccardin A (3), riccardin A (1), and riccardin B (4) were synthesized by convergent schemes.Rings A and D of both riccardin A and B, as well as rings B and C of riccardin B were joined by the Ullmann ether synthesis.The aryl-aryl bond in ricca
- Gottsegen, Agnes,Nogradi, Mihaly,Vermes, Borbala,Kajtar-Peredy, Maria,Bihatsi-Karsai, Eva
-
p. 315 - 320
(2007/10/02)
-
- THE CONSTITUTION OF RICCARDIN B
-
The constitution of riccardin B, a macrocyclic bis(bibenzyl) isolated from Riccardia multifida was established by unambigous synthesis of its di-O-methyl ether.
- Nogradi, M.,Vermes, B.,Kajtar-Peredy, M.
-
p. 2899 - 2900
(2007/10/02)
-