210992-90-8Relevant academic research and scientific papers
Synthesis and biological evaluation of novel anticancer bivalent colchicine-tubulizine hybrids
Malysheva, Yulia B.,Combes, Sebastien,Allegro, Diane,Peyrot, Vincent,Knochel, Paul,Gavryushin, Andrei E.,Fedorov, Alexey Yu.
experimental part, p. 4271 - 4278 (2012/08/28)
A series of novel antimitotic hybrids were synthesized in good yields by linking of azide-containing colchicine congeners with acetylene-substituted tubulizine-type derivatives using copper-mediated 1,3-dipolar cycloaddition. Obtained compounds exhibit go
Identification of 12Cysβ on tubulin as the binding site of tubulyzine
Kim, Yeoun Jin,Sackett, Dan L.,Schapira, Matthieu,Walsh, Daniel P.,Min, Jaeki,Pannell, Lewis K.,Chang, Young-Tae
, p. 1169 - 1175 (2007/10/03)
We have undertaken quantitative binding site studies in order to identify the binding site of the known microtubule destabilizing agents, the tubulyzines, in the tubulin dimer. Two different approaches were employed that utilized the tubulyzines and their
A novel microtubule destabilizing entity from orthogonal synthesis of triazine library and zebrafish embryo screening
Moon, Ho-Sang,Jacobson, Eric M.,Khersonsky, Sonya M.,Luzung, Michael R.,Walsh, Daniel P.,Xiong, Wennan,Lee, Jae Wook,Parikh, Puja B.,Lam, Jennifer C.,Kang, Tae-Wook,Rosania, Gustavo R.,Schier, Alexander F.,Chang, Young-Tae
, p. 11608 - 11609 (2007/10/03)
The first orthogonal combinatorial synthesis of a high-purity triazine library was demonstrated. Novel triazine-based microtubule inhibitors were discovered by an efficient zebrafish embryo screening and in vitro microtubule polymerization assay. Copyrigh
Pyrazole derivatives
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, (2019/07/22)
The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.
