157425-30-4Relevant academic research and scientific papers
Synthesis, cytotoxic activity and binding model analysis of novel isoxazole-docetaxel analogues with C3′-N modification
Chen, Ming,Liu, Jiyuan,Tian, Zhen,Liu, Xueying,Zhang, Shengyong
, p. 1355 - 1365 (2018/04/10)
Structure–activity relationship (SAR) studies confirm that modifications at C-3′ position can lead to the development of highly potent novel taxoids. We designed and synthesized a series of novel isoxazole-docetaxel analogues A1–A5 by introducing isoxazol
Taxane anti-tumor drug KABA docetaxel synthesis method
-
Paragraph 0036-0038, (2017/08/25)
The invention relates to a novel synthesis method of taxane antitumor drug cabazitaxel. The method relates to six-step reaction. Firstly, a key intermediate compound 7 as shown in the specification is obtained, and then reacts with di-tert-butyl dicarbonate ester (Boc)2O, so as to obtain the final product cabazitaxel. The whole reaction process does not relate to low-temperature operation and column chromatography purification, and the method is easy to operate, convenient to purify, and easy in mass production.
Synthesis and Antifeedant Properties of N-Acylphenylisoserinates of Lactarius Sesquiterpenoid Alcohols
Kopczacki,Gumulka,Masnyk,Sarosiek,Barycki,Ignacak,Zochowski,Grabarczyk,Nowak,Daniewski
, p. 89 - 108 (2007/10/03)
The esterification of various sesquiterpenoid alcohols of Lactarius origin with N-benzoyl-[2R,3S]-phenylisoserine (side chain of Taxol), N-acetyl-[2R,3S]-phenylisoserine and N-tert-butoxy-[2R,3S]-phenylisoserine (side chain of Taxotere) produced compounds whose antifeedant properties against storage pests Tribolium confusum, Trogoderma granarium, Sitophylus granarius and Rhizoperta dominica were measured. The introduction of the ester moiety in these molecules, in comparison to original compounds, moderately enhanced their antifeedant activities, as well as changed their selectivity of activity towards the test insects.
A novel approach of water-soluble paclitaxel prodrug with no auxiliary and no byproduct: Design and synthesis of isotaxel
Hayashi, Yoshio,Skwarczynski, Mariusz,Hamada, Yoshio,Sohma, Youhei,Kimura, Tooru,Kiso, Yoshiaki
, p. 3782 - 3784 (2007/10/03)
A novel water-soluble paclitaxel prodrug, isotaxel 2, that realizes a higher water-solubility and the formation of paclitaxel through a simple pH-dependent chemical mechanism via the O-N acyl migration was synthesized and showed promising results in water
Synthesis and cytotoxic properties of N-Boc-phenylisoserinates of sesquiterpenoic alcohols from mushrooms of Lactarius genus, as analogues of Taxotere
Sarosiek,Masnyk,Gumulka,Daniewski,Kobus,Krawczyk,Luczak
, p. 73 - 82 (2007/10/03)
Sesquiterpenoic analogues of Taxotere i.e., N-BOC-phenylisoserinates of sesquiterpenoic alcohols, isolated from mushrooms of Lactarius genus, were synthesized. Cytotoxicity of compounds, thus obtained, was evaluated using Vero cells.
Method of preparing taxane derivatives
-
, (2008/06/13)
This invention relates to a method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), elimination of protection groupings of the ester obtained, and acylation of the amine function of the side chain. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R1 is benzoyl or R2 --CO--O-- in which R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R3 and R4 may be the same or different and represent hydrogen, alkyl, alkenyl, aralkyl, aryl or alkoxy, and R5 is an alkyl radical substituted by one or more chlorine atoms (2,2,2-trichloroethyl, (2-trichloromethylisopropyl). STR1
