Synthesis and some transformations of 6(8)-substituted 4-hydrazino-2-methylquinolines
摘要:
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]quinolines and 4-(5-ethoxy-3-methyl-1H-pyrazol-1-yl)-2-methylquinolines.
Synthesis and some transformations of 6(8)-substituted 4-hydrazino-2-methylquinolines
摘要:
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]quinolines and 4-(5-ethoxy-3-methyl-1H-pyrazol-1-yl)-2-methylquinolines.
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard–quinoline conjugates having a urea or hydrazinecarboxamide linker
作者:Rajesh Kakadiya、Huajin Dong、Amit Kumar、Dodia Narsinh、Xiuguo Zhang、Ting-Chao Chou、Te-Chang Lee、Anamik Shah、Tsann-Long Su
DOI:10.1016/j.bmc.2010.01.061
日期:2010.3
A series of N-mustard-quinoline conjugates bearing a urea or hydrazinecarboxamide linker was synthesized for antitumor evaluation. The in vitro cytotoxicity studies revealed that compounds with hydrazinecarboxamide linkers were generally more cytotoxic than the corresponding urea counterparts in inhibiting human lymphoblastic leukemia and various solid tumor cell growths in culture. The therapeutic efficacy against human tumor xenografts in animal model was studied. It was shown that complete tumor remission in nude mice bearing human breast carcinoma MX-1 xenograft by 17a, i and 18c, d was achieved. In the present study, it was revealed that both linkers are able to lower the chemically reactive N-mustard pharmacophore and thus the newly synthesized conjugates possess a long half-life in rat plasma. Moreover, the new N-mustard derivatives are able to induce DNA cross-linking either by modified comet assay or by alkaline agarose gel shift assay. (C) 2010 Elsevier Ltd. All rights reserved.
ANILINOPYRAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DIABETES
申请人:Bayer HealthCare, LLC
公开号:EP1928455A1
公开(公告)日:2008-06-11
[EN] ANILINOPYRAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DIABETES<br/>[FR] DERIVES D'ANILINOPYRAZOLE UTILISES DANS LE TRAITEMENT DU DIABETE
申请人:BAYER PHARMACEUTICALS CORP
公开号:WO2007027842A1
公开(公告)日:2007-03-08
[EN] The present invention relates to anilinopyrazole compounds of formula (1) in which R3 represents an aromatic 5- or 6-membered heteroaromatic ring which is optionally fused to phenyl, said heterocycle or fused heterocycle is optionally substituted, X represents a carboxylic acid, ester or amide, or sulfonamide, and the remaining groups are as defined in the text. It also relates to pharmaceutical compositions containing these materials and, and methods for treating diabetes and related disorders using these materials. [FR] La présente invention concerne des composés d'anilinopyrazole représentés par la formule (I) dans laquelle R3 désigne un noyau hétéroaromatique à 5 ou 6 chaînons qui est éventuellement fusionné à phényle, ledit hétérocycle ou hétérocycle fusionné étant éventuellement substitué, X désigne acide carboxylique, ester ou amide, ou sulfonamide et les groupes restants sont tels que définis dans la description. Cette invention concerne également des compositions pharmaceutiques contenant ces matériaux ainsi que des méthodes permettant de traiter le diabète et des troubles associés à l'aide de ces matériaux.
Synthesis and some transformations of 6(8)-substituted 4-hydrazino-2-methylquinolines
作者:A. A. Avetisyan、I. L. Aleksanyan、L. P. Ambartsumyan
DOI:10.1134/s107042801003022x
日期:2010.3
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]quinolines and 4-(5-ethoxy-3-methyl-1H-pyrazol-1-yl)-2-methylquinolines.