1433192-31-4Relevant academic research and scientific papers
A gulose moiety contributes to the belomycin (BLM) disaccharide selective targeting to lung cancer cells
Cao, Yongjun,Chen, Wenming,Huang, Weiping,Li, Houkai,Liao, Guohao,Qi, Dongxia,Wang, Meizhu,Wang, Xiaoyang,Ye, Wenchong,Zhou, Cui,Zhou, Wen
, (2021/10/07)
Eight mono- or disaccharide analogues derived from BLM disaccharide, along with the corresponding carbohydate-dye conjugates have been designed and synthesized in this study, aiming at exploring the effect of a gulose residue on the cellular binding/uptake of BLM disaccharide and it possible uptake mechanism. Our evidence is presented indicating that, for the cellular binding/uptake of BLM disaccharide, a gulose residue is an essential subunit but unrelated to its chemical nature. Interestingly, D-gulose-dye conjugate is able to selectively target A549 cancer cells, but L-gulose-dye conjugate fails. Further uptake mechanism studies demonstrate D-gulose-dye derivatives similar to BLM disaccharide-dye ones behave in a temperature- and ATP-dependent manner, and are partly directed by the GLUT1 receptor. Moreover, D-gulose modifying gemcitabine 53a exhibits more potent antitumor activity compared to derivatives 53b-c in which gemcitabine is decorated with other monosaccharides. Taken together, the monosacharide D-gulose conjugate offers a new strategy for solving cytotoxic drugs via the increased tumor targeting in the therapy of lung cancer.
Oligosaccharide-camptothecin conjugates as potential antineoplastic drugs: Design, synthesis and biological evaluation
Li, Maolin,Ye, Wenchong,Fu, Kaishuo,zhou, Cui,Shi, Yonghui,Huang, Weiping,Chen, Wenming,Hu, Jiliang,Jiang, Zhilin,Zhou, Wen
, (2020/07/15)
Thirty novel 20 (S)–O-linked camptothecin (CPT) glycoconjugates were synthesized. They showed more potent in vitro cytotoxicities over irinotecan, but very weak direct topoisomerase I (Topo I) inhibition was observed at 100.0 μM. Oligosaccharide types, length of a PEG linker and acetyl groups exerted obvious effects on cytotoxicity, selectivity, water solubility and stability of the newly synthesized CPT glycoconjugates. Construct 40, with a bleomycin (BLM) disaccharide linked to diethylene glycol in the introduced ester moiety, demonstrated a superior antitumor activity and a distinct selectivity compared to CPT. No toxicity was detectable in animal acute toxicity intravenously (160 mg/kg). Collectively, attachment of oligosaccharides with tumor targeting to 20 (S)–OH of CPT could offer a solution to the daunting problems posed by current Topo I poisons.
Tenofovir derivative and preparation method and application thereof
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, (2019/11/12)
The invention discloses a tenofovir derivative and a preparation method and application thereof and belongs to the technical field of antiviral drugs. The tenofovir derivative has antiviral effect, can be enriched in the liver and slowly release active co
Dynamic multivalency for carbohydrate-protein recognition through dynamic combinatorial libraries based on FeII-bipyridine complexes
Reeh, Philipp,De Mendoza, Javier
supporting information, p. 5259 - 5262 (2013/05/09)
Molecular recognition: Dynamic combinatorial libraries (DCLs) exploiting multivalency effects and metal coordination have been employed for carbohydrate-protein recognition. The interaction of a three-component DCL based on 2,2′-bipyridine (bipy)-FeII complexes with concanavalin A (ConA; see scheme) results in enhanced binding by multivalent presentation with a bias towards mannose-containing library components. Copyright
