53117-14-9Relevant articles and documents
Design, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as novel microtubule destabilizers
Wang, Chao,Li, Yuelin,Liu, Zi,Wang, Zeyu,Liu, Zihan,Man, Shuai,Zhang, Yujing,Bao, Kai,Wu, Yingliang,Guan, Qi,Zuo, Daiying,Zhang, Weige
, p. 549 - 560 (2021/02/05)
A series of 1-aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as microtubule destabilizers were designed, synthesised and evaluated for anticancer activity. Based on bioisosterism, we introduced the tetrazole moiety containing the hydrogen-bond acceptors as B-ring of XRP44X analogues. The key intermediates ethyl 1-aryl-1H-tetrazole-5-carboxylates 10 can be simply and efficiently prepared via a microwave-assisted continuous operation process. Among the compounds synthesised, compound 6–31 showed noteworthy potency against SGC-7901, A549 and HeLa cell lines. In mechanism studies, compound 6–31 inhibited tubulin polymerisation and disorganised microtubule in SGC-7901 cells by binding to tubulin. Moreover, compound 6–31 arrested SGC-7901cells in G2/M phase. This study provided a new perspective for development of antitumor agents that target tubulin.
Synthesis and biological evaluation of novel oxalamido derivatives as caspase-3 inhibitors
Sengupta, Saumitra,Rao, G. Venkateshwar,Dubey
body text, p. 901 - 905 (2011/09/12)
A new series of 5-fluoro-3-[(4-substituted-phenylaminooxalyl)-amino]-4-oxo- pentanoic acid, 7a-c, 3-[(4-substitutedphenylaminooxalyl)- amino]-4-oxo-5-(2,3, 5,6-tetrafluoro-phenoxy)-pentanoic acid, 7d-h and 5-(2,6-difluoro-phenoxy)-3- [(substituted-phenylaminooxalyl)-amino]-4-oxo-pentanoic acid, 7i-p have been synthesized from N-(substituted-phenyl)- oxalamic acid, 1 and their activities have been evaluated in vitro. Compounds 7b,c and k show low micromolar inhibitory activity against caspase-3.
Ligand design for heterobimetallic single-chain magnets: Synthesis, crystal structures, and magnetic properties of MIICuII (M = Mn, Co) chains with sterically hindered methyl-substituted phenyloxamate bridging ligands
Pardo, Emilio,Ruiz-Garcia, Rafael,Lloret, Francesc,Faus, Juan,Julve, Miguel,Journaux, Yves,Novak, Miguel A.,Delgado, Fernando S.,Ruiz-Perez, Catalina
, p. 2054 - 2066 (2008/02/04)
Two new series of neutral oxamato-bridged heterobimetallic chains of general formula [MCu(Lx)2]· mDMSO (m = 0-4) (L 1 = N-2-methyl-phenyloxamate, M = Mn (1a) and Co (1b) ; L2 = N-2,6-dimethylphenyloxamate, M = M