Synthesis, antiproliferative and antibacterial evaluation of C-ring modified colchicine analogues
A series of 10 amine derivatives of colchicine have been obtained with high yields by modification at C(10)-OCH3position of C-ring and characterized by spectroscopic methods. In vitro cytotoxicity has been evaluated against four human tumour ce
Huczyński, Adam,Rutkowski, Jacek,Popiel, Katarzyna,Maj, Ewa,Wietrzyk, Joanna,Stefańska, Joanna,Majcher, Urszula,Bartl, Franz
Colchicine derivatives with potent anticancer activity and reduced P-glycoprotein induction liability
Colchicine (1), a nature-derived microtubule polymerization inhibitor, develops multi-drug resistance in tumor cells due to its P-gp substrate and induction activity, which in turn leads to its rapid efflux from tumor cells. This auto-induction of the eff
Synthesis and antitumour activity of novel colchicine C-10 derivatives
A series of new colchicine C-10 derivatives (2a-i, 3a-h) were synthesized by replacement of the 10-methoxy with NR2 and SCH3 in order to determine their cytotoxic activity. The compounds were synthesized in good yield and the structures of all newly synthesized compounds were established on the basis of their IR, 1H NMR and elemental analysis. The synthesized compounds were tested in vitro antitumor activity against four human cancer cell lines by MTT assay. It was found that many of the derivatives displayed significant activity, particularly, compound 2a and 2b showed more potent cytotoxic activities than colchicine.
Shen, Li Hong,Zhang, Le,Wang, Hai Xian,Wang, Xin,Zhang, Gai Jiao
p. 7475 - 7476
(2015/04/22)
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