87304-15-2Relevant articles and documents
Design, synthesis and biological evaluation of hybrid of ubenimex-fluorouracil for hepatocellular carcinoma therapy
Hou, Xiaohan,Jia, Geng,Jiang, Yuqi,Li, Peixia,Li, Xiaoyang,Tan, Leqiao,Wang, Xuejian,Xu, Wenfang,Yue, Kairui,Zhang, Jian,Zhang, Liang,Zhang, Zhaolin
, (2021/09/22)
In our previous study, we discovered a ubenimex-fluorouracil (5FU) conjugates BC-02, which displays significant in vivo anti-tumor activity, however, the instability of BC-02 in plasma limits its further development as a drug candidate. Herein, we designe
TUBULIN BINDING AGENTS
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Paragraph 1083; 1084; 1085; 1086; 1087, (2015/02/18)
The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene. The second substituent on the B ring may for example be a substituent which has been found to provide enhanced tubulin binding activity (for example a carbonyl group), or may be a substituent that facilitates functionalisation of the B ring (for example an hydroxyl or amine group), or it may be a binding agent for a target that is preferentially expressed on vasculature undergoing angiogenesis, and not expressed on quiescent vasculature.
Development of target protein-selective degradation inducer for protein knockdown
Itoh, Yukihiro,Ishikawa, Minoru,Kitaguchi, Risa,Sato, Shinichi,Naito, Mikihiko,Hashimoto, Yuichi
experimental part, p. 3229 - 3241 (2011/06/25)
Our previous technique for inducing selective degradation of target proteins with ester-type SNIPER (Specific and Nongenetic Inhibitor-of-apoptosis- proteins (IAPs)-dependent Protein ERaser) degrades both the target proteins and IAPs. Here, we designed a