656233-42-0Relevant articles and documents
Synthesis and antitumor activity evaluation of a novel series of camptothecin analogs
Lv, Jian,Guo, Na,Wen, Shao-Peng,Teng, Yu-Ou,Ma, Meng-Xin,Yu, Peng
, p. 867 - 874 (2013)
A series of novel 10-substituted camptothecin analogs (3-10) with a carbamate linker were synthesized, and their biological activities were evaluated. The amino acid-linked carbamate derivatives (8-10) of the camptothecin-type natural product not only pos
Synthesis and biological evaluation of novel water-soluble poly-(ethylene glycol)-10-hydroxycamptothecin conjugates
Guo, Na,Jiang, Du,Wang, Luyao,You, Xing,Teng, Yu-Ou,Yu, Peng
, p. 9393 - 9404 (2015)
In order to improve the antitumor activity and water solubility of 10-hydroxycamptothecin (HCPT), a series of novel HCPT conjugates were designed and synthesized by conjugating polyethylene glycol (PEG) to the 10-hydroxyl group of HCPT via a valine spacer
Multi-gram scale synthesis of a bleomycin (BLM) carbohydrate moiety: exploring the antitumor beneficial effect of BLM disaccharide attached to 10-hydroxycamptothecine (10-HCPT)
Li, MaoLin,Huang, Weiping,Jiang, Zhilin,Shi, Yonghui,Yuan, Sisi,Fu, Kaishuo,Chen, YongJun,Zhou, Li,Zhou, Wen
, p. 6010 - 6020 (2019/04/17)
The “tumor-seeking” role of bleomycin (BLM) disaccharide has been demonstrated to serve as a promising tool for cancer diagnosis and a potential ligand for targeted therapy. However, these practical applications are often hampered by the lack of BLM disaccharide. Herein, an efficient multi-gram synthesis of peracetylated BLM disaccharide 20 is achieved by a TMSOTF-mediated glycosidation coupling manner in 43.6% overall yield in terms of benzyl galactoside. The critical innovation of the synthetic strategy is that inexpensive benzyl galactoside was first adopted to prepare an l-gulose subunit 3 as a glycosyl acceptor, with a much shorter route in 73.0% yield, and a 3-O-carbamoyl-mannose donor 4 was achieved in 47.2% yield by lowering the amount of dibutyltin oxide, and merging aminolysis and selective deacetylation into a one-pot reaction. Next, the incorporation of BLM disaccharide into 10-hydroxycamptothecin (10-HCPT), a non-specific model compound, to form conjugate 1 could significantly improve the antitumor activity and display obvious selectivity toward cancerous and normal cells in comparison with 10-HCPT. Moreover, BLM disaccharide itself was non-cytotoxic, clearly indicating the importance and potential of BLM disaccharide in solving the targeted antitumor therapy of cytotoxic drugs.
Camptothecin sugar derivative and preparation method and application thereof
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Paragraph 0051-0053, (2019/11/13)
The invention relates to a camptothecin sugar derivative and a preparation method and application thereof, and belongs to the field of biological medicines. The structural formula of the camptothecinsugar derivative is shown in formula (I) in specification. The camptothecin sugar derivative can obviously improve the stability and water solubility of camptothecin and 10-hydroxycamptothecin, and has different sensitivities to different tumor cells. Especially when the chain link n equals to 1, the camptothecin sugar derivative of the invention can significantly increase the selectivity to tumorcells.
Synthesis and evaluation of a DHA and 10-hydroxycamptothecin conjugate
Wang, Yuqiang,Li, Lianfa,Jiang, Wei,Larrick, James W.
, p. 5592 - 5599 (2007/10/03)
We have synthesized a conjugate of cis-4,7,10,13,16,19-docosahexenoic acid (DHA) and 10-hydroxycamptothecin (HCPT), DHA-HCPT. The antitumor activity of DHA-HCPT was evaluated in vitro against L1210 leukemia cells and in experimental animal tumor models in
Novel anticancer conjugates of camptothecin and unsaturated fatty acids
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Page/Page column 12; Sheet 2, (2008/06/13)
The present invention provides novel conjugates of camptothecin compounds and long-chain unsaturated fatty acid. The novel conjugates can be used to treat mammalian cell proliferative diseases such as cancer.