3123-89-5Relevant academic research and scientific papers
Synthesis, antiproliferative activity and molecular docking of Colchicine derivatives
Huczyński, Adam,Majcher, Urszula,Maj, Ewa,Wietrzyk, Joanna,Janczak, Jan,Moshari, Mahshad,Tuszynski, Jack A.,Bartl, Franz
, p. 103 - 112 (2016)
In order to create more potent anticancer agents, a series of five structurally different derivatives of Colchicine have been synthesised. These compounds were characterised spectroscopically and structurally and their antiproliferative activity against f
Synthesis, Biological Evaluation, and Molecular Docking of Combretastatin and Colchicine Derivatives and their hCE1-Activated Prodrugs as Antiviral Agents
Richter, Michael,Boldescu, Veaceslav,Graf, Dominik,Streicher, Felix,Dimoglo, Anatoli,Bartenschlager, Ralf,Klein, Christian D.
, p. 469 - 483 (2019/02/01)
Recent studies indicate that tubulin can be a host factor for vector-borne flaviviruses like dengue (DENV) and Zika (ZIKV), and inhibitors of tubulin polymerization such as colchicine have been demonstrated to decrease virus replication. However, toxicity limits the application of these compounds. Herein we report prodrugs based on combretastatin and colchicine derivatives that contain an ester cleavage site for human carboxylesterase, a highly abundant enzyme in monocytes and hepatocytes targeted by DENV. Relative to their parent compounds, the cytotoxicity of these prodrugs was reduced by several orders of magnitude. All synthesized prodrugs containing a leucine ester were hydrolyzed by the esterase in vitro. In contrast to previous reports, the phenylglycine esters were not cleaved by human carboxylesterase. The antiviral activity of combretastatin, colchicine, and selected prodrugs against DENV and ZIKV in cell culture was observed at low micromolar and sub-micromolar concentrations. In addition, docking studies were performed to understand the binding mode of the studied compounds to tubulin.
Colchicine derivatives with potent anticancer activity and reduced P-glycoprotein induction liability
Singh, Baljinder,Kumar, Ashok,Joshi, Prashant,Guru, Santosh K.,Kumar, Suresh,Wani, Zahoor A.,Mahajan, Girish,Hussain, Aashiq,Qazi, Asif Khurshid,Kumar, Ajay,Bharate, Sonali S.,Gupta, Bishan D.,Sharma, Parduman R.,Hamid, Abid,Saxena, Ajit K.,Mondhe, Dilip M.,Bhushan, Shashi,Bharate, Sandip B.,Vishwakarma, Ram A.
, p. 5674 - 5689 (2015/05/27)
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
Antitumor agents. Part 186: Synthesis and biological evaluation of demethylcolchiceinamide analogues as cytotoxic DNA topoisomerase II inhibitors
Guan, Jian,Zhu, Xiao-Kang,Tachibana, Yoko,Bastow, Kenneth F.,Brossi, Arnold,Hamel, Ernest,Lee, Kuo-Hsiung
, p. 2127 - 2131 (2007/10/03)
Demethylation of colchiceinamide (2) and its analogues (3-10) afforded a novel class of mammalian DNA topoisomerase II inhibitors (2a-10a) without displaying tubulin inhibitory activity. All target compounds inhibited the catalytic activity of topoisomera
