26437-22-9Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of a Novel Water-soluble Prodrug of Docetaxel with Amino Acid as a Linker
Ma, Huan,Chen, Gang,Wang, Tao,Li, Qingeng,Liu, Yan
, p. 363 - 369 (2016)
The synthesis and preliminary evaluation of derivatives of docetaxel with novel amino acid as a linker named as LK-193?LK-196 was described. The C2′-modified compound LK-196 behaves as a prodrug; that is, docetaxel is generated upon exposure to human plasma. The compound was also found to have greatly improved water solubility. The pharmacodynamic results showed LK-196 had the self-evident inhibitory effect on tumor growth in vivo, which is a promising candidate for further biological evaluation.
Industrial synthesis method of water-soluble docetaxel derivative
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Paragraph 0377-0383, (2022/01/10)
The invention provides an industrial synthesis method of a water-soluble docetaxel derivative. The method is characterized in that 10-deacetylbaccatin III is used as a substrate, and the 10-deacetylbaccatin III and (R)-4-dimethylamino-2-fluoro-butyric acid hydrochloride are synthesized into the water-soluble docetaxel derivative. According to the method, a two-step synthesis technology, a centrifugal extraction separation technology, a recrystallization technology, a supercritical CO2 fluid drying technology and a full-automatic control technology are combined, synthesis and purification are carried out under the synergistic effect of the technologies, the water solubility of the water-soluble docetaxel derivative produced by the combined technology can reach 12 mg/ml or above, and the the water-soluble docetaxel derivative has about 2000 times higher solubility in water than docetaxel. A docetaxel injection prepared by the method does not use absolute ethyl alcohol or Tween-80 hydrotropy, and the docetaxel derivative is a water-soluble docetaxel derivative which is efficient, free of anaphylactic reaction and small in toxic and side effect. Therefore, the product has the characteristics of small toxic and side effects, low production cost, high product purity, high product yield and stable quality, and is suitable for industrial large-scale production.
DNA sequence selectivity of hairpin polyamide turn units
Farkas, Michelle E.,Li, Benjamin C.,Dose, Christian,Dervan, Peter B.
supporting information; experimental part, p. 3919 - 3923 (2010/03/02)
A class of hairpin polyamides linked by 3,4-diaminobutyric acid, resulting in a β-amine residue at the turn unit, showed improved binding affinities relative to their α-amino-γ-turn analogs for particular sequences. We incorporated β-amino-γ-turns in six-
