65764-56-9Relevant articles and documents
Rational Design, Synthesis and Evaluation of Indole Nitrogen Hybrids as Photosystem II Inhibitors
de Souza, Jéssica Maria,Fazolo, Bruno Rodrigues,Lacerda, Jhully Wellen Ferreira,Moura, Mariana de Souza,dos Santos, Arielly Celestino Rodrigues,de Vasconcelos, Leonardo Gomes,de Sousa Junior, Paulo Teixeira,Dall’Oglio, Evandro Luiz,Ali, Akbar,Sampaio, Olívia Moreira,Vieira, Lucas Campos Curcino
, p. 1233 - 1242 (2020/07/06)
We report the synthesis of twelve indole derivatives bearing nitro or amide groups via Fischer indole methodology followed by reduction/acetylation and amidation reactions. After thorough characterization, these indoles were subjected to a number of studies in order to evaluate their bioactive potential as photosynthesis and plant growth inhibitors. Firstly, these molecular hybrids were evaluated as photosystem II (PSII) inhibitors through chlorophyll a (Chl a) fluorescence measurement. In this study, 6-chloro-8-nitro-2,3,4,9-tetrahydro-1H-carbazole (15a) and 5-chloro-2,3-dimethyl-7-nitro-1H-indole (15b) showed the best results by reducing the phenomenological parameters of reaction centers ABS/RC, TR0/RC and ET0/RC of PSII. Electron chain blockage by these compounds may lead to diminished ATP synthesis and CO2 fixation which interrupt the plant development. The compounds 15a and 15b both act as postemergent herbicides, reducing the dry biomass of Ipomoea grandifolia and Senna alata weeds by an average of 40% and 37%, respectively, corroborating the fluorescence results. Additionally, the molecular docking study revealed that the presence of strong electron-withdrawing groups at the indole phenyl ring is important for the ligand’s interaction with the binding pocket of protein D1 on PSII. The optimization of these molecular features is the goal of our research group in further understanding and development of new potent herbicides.
N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors
Barf, Tjeerd,Lehmann, Fredrik,Hammer, Kristin,Haile, Saba,Axen, Eva,Medina, Carmen,Uppenberg, Jonas,Svensson, Stefan,Rondahl, Lena,Lundbaeck, Thomas
scheme or table, p. 1745 - 1748 (2010/02/28)
Small molecule inhibitors of adipocyte fatty-acid binding protein (A-FABP) have gained renewed interest following the recent publication of pharmacologically beneficial effects of such inhibitors. Despite the potential utility of selective A-FABP inhibito
Synthesis and evaluation of novel pyrimido-acridone, -phenoxadine, and -carbazole as topoisomerase II inhibitors
Kamata, Junichi,Okada, Toshimi,Kotake, Yoshihiko,Niijima, Jun,Nakamura, Katsuji,Uenaka, Toshimitsu,Yamaguchi, Atsumi,Tsukahara, Kappei,Nagasu, Takeshi,Koyanagi, Nozomu,Kitoh, Kyosuke,Yoshimatsu, Kentaro,Yoshino, Hiroshi,Sugumi, Hiroyuki
, p. 1071 - 1081 (2007/10/03)
As part of a series of studies to discover new topoisomerase II inhibitors, novel pyrimidoacridones, pyrimidophenoxadines, and pyrimidocarbazoles were synthesized, and in vitro and in vivo antitumor activities and DNA-protein and/or DNA-topoisomerase II c
