110455-07-7

Upstream product

• 5557-81-3 L-alanine benzyl ester hydrochloride 
• 503-38-8 trichloromethyl chloroformate 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 42854-62-6 L-alanine benzyl ester p-toluenesulfonate 

Downstream Products

• 109953-20-0 C₂₇H₄₂N₆O₈ 

Relevant academic research and scientific papers

Taxol-DHA-dextran coupling polymer, synthetic method thereof and application of polymer

The invention provides a taxol-DHA-dextran coupling polymer, a synthetic method thereof and an application of the polymer, and belongs to the technical field of biological medicines. According to thepolymer, polysaccharides serve as polymer drug-loaded frameworks, so that an anti-tumor drug-polysaccharide passive targeted coupling polymer is prepared, taxol can be passively targeted into a tumortissue by the aid of an EPR effect, and an anti-tumor function is played. Water solubility and biocompatibility of taxol medicines can be increased, accumulation of anti-tumor medicines in the tumor tissue can be increased under the passive targeted action, general side effect and nervous side effect of the taxol medicines are reduced, and the polymer has good practical application values.

Synthesis and biological evaluation of novel 10-substituted-7- Ethyl-10-hydroxycamptothecin (SN-38) prodrugs

In an attempt to improve the antitumor activity and reduce the side effects of irinotecan (2), novel prodrugs of SN-38 ( 3) were prepared by conjugating amino acids or dipeptides to the 10-hydroxyl group of SN-38 via a carbamate linkage. The synthesized compounds completely generated SN-38 in pH 7.4 buffer or in human plasma, while remaining stable under acidic conditions. All prodrug compounds demonstrated much greater in vitro antitumor activities against HeLa cells and SGC-7901 cells than irinotecan. The most active compounds, 5h, 7c, 7d, and 7f, exhibited IC50 values that were 1000 times lower against HeLa cells and 30 times lower against SGC-7901 cells than those of irinotecan, and the inhibitory activities of these prodrugs against acetylcholinesterase (AchE) were significantly reduced, with IC50 values more than 6.8 times greater than that of irinotecan. In addition, compound 5e exhibited the same level of tumor growth inhibitory activity as irinotecan (CPT-11) in a human colon xenograft model in vivo.