49612-00-2Relevant academic research and scientific papers
Solid-supported hydrazone of 4-(4′-Formyl-3′-methoxyphenoxy)butyric acid as a new traceless linker for solid-phase synthesis
Okorochenkov, Sergei,Burglova, Kristyna,Popa, Igor,Hlavac, Jan
supporting information, p. 180 - 183 (2015/01/30)
The use of a hydrazine derived from a backbone amide linker as a new hydrazone-based traceless linker for solid-phase organic synthesis is described. The stability of the linker was tested under various conditions, including treatment with acids, bases, and borohydrides. Final compounds can be released by selective cleavage using trimethylsilanolate. To demonstrate the versatility of the linker, the synthesis of a model compound under various reaction conditions was performed with good results.
N1-{4-[(10S)-Dihydroartemisinin-10-oxyl]}phenylmethylene-N 2-(2-methylquinoline-4-yl)hydrazine derivatives as antiplasmodial falcipain-2 inhibitors
Luo, Wei,Liu, Yang,Wang, Jian,Guo, Chun,Lu, Wei-Qiang,Cui, Kun-Qiang
, p. 3073 - 3079,7 (2020/08/20)
A series of N1-{4-[(10S)-dihydroartemisinin- 10-oxyl]}phenylmethylene-N2-(2-methylquinoline-4-yl) hydrazine derivatives 9a-9n possessing 4-quinolylhydrazone and artemisinin cores were herein synthesized and evaluated for their activities against cysteine protease falcipain- 2 of Plasmodium falciparum. The structures were clearly confirmed by elemental analysis, 1H NMR, and mass spectra. The pharmacological results indicated that all compounds showed excellent activity against recombinant falcipain-2 (IC50 = 0.15-2.28 μM). The best one of this series was compound 9d (IC50 = 0.15 μM). The molecular docking results showed that the compound 9d made close contact with the key active site of cysteine protease falcipain-2.
Synthesis and some transformations of 6(8)-substituted 4-hydrazino-2- methylquinolines
Avetisyan,Aleksanyan,Ambartsumyan
experimental part, p. 427 - 431 (2010/09/20)
6(8)-Substituted 4-hydrazino-2-methylquinolines were synthesized by reaction of the corresponding 4-chloro-2-methylquinolines with hydrazine hydrate. Reactions of the title compounds with ethyl acetoacetate and acetone gave 2,4-dimethyl-1H-pyrrolo[3,2-c]q
ANILINE OR PHENOL MUSTARDS LINKED TO DNA-AFFINIC MOLECULES OR WATER-SOLUBLE AROMATIC RINGS AND THEIR USE AS CANCER THERAPEUTIC AGENTS
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Page/Page column 20, (2008/12/06)
New aniline or phenol N-mustards linked to DNA-affinity carriers (such as 9-anilinoacridines, acridines andquinolines), aminobenzamides or aminophenol ethers by a urea, carbamic acid, carbanic acid ester, hydxazine urea, hydrazine carbamic acid ester, phenoxyurea, phenoxycarbamic acid ester linkage with improved chemical stability and anti-tumor therapeutic efficacy are provided.
