928064-05-5Relevant academic research and scientific papers
Synthesis of new secretory phospholipase A2-inhibitory indole containing isoxazole derivatives as anti-inflammatory and anticancer agents
Pedada, Srinivasa Rao,Yarla, Nagendra Sastry,Tambade, Pawan J.,Dhananjaya, Bhadrapura Lakkappa,Bishayee, Anupam,Arunasree, Kalle M.,Philip, Gundala Harold,Dharmapuri, Gangappa,Aliev, Gjumrach,Putta, Swathi,Rangaiah, Gururaja
, p. 289 - 297 (2018/04/19)
Secretory phospholipase A2 (sPLA2) is an important enzyme that plays a key role in various inflammatory diseases including cancer and its inhibitors have been developed as preventive or therapeutic agents. In the present study, a series of new indole containing isoxazole derivatives (10a–10o) is synthesized and evaluated for their sPLA2 inhibitory activities. All compounds (10a–10o) showed significant sPLA2 inhibition activities both in vitro and in vivo studies which is substantiated in in silico studies. Among all the tested compounds, 10o showed potent sPLA2 inhibition activity, that is comparable or more to ursolic acid (positive control). Further studies demonstrated that 10o showed in vitro antiproliferative activity when tested against MCF-7 breast and DU145 prostate cancer cells. Furthermore, compounds 10a–10o obeyed lipinsky's rule of 5 and suggesting druggable properties. The in vitro, in vivo and in silico results are encouraging and warrant pre-clinical studies to develop sPLA2-inhibitory compound 10o as novel therapeutic agent for various inflammatory disorders and several malignancies.
4-Azolylphenyl isoxazoline insecticides acting at the GABA gated chloride channel
Lahm, George P.,Cordova, Daniel,Barry, James D.,Pahutski, Thomas F.,Smith, Ben K.,Long, Jeffrey K.,Benner, Eric A.,Holyoke, Caleb W.,Joraski, Kathleen,Xu, Ming,Schroeder, Mark E.,Wagerle, Ty,Mahaffey, Michael J.,Smith, Rejane M.,Tong, My-Hahn
, p. 3001 - 3006 (2013/06/26)
Isoxazoline insecticides have been shown to be potent blockers of insect GABA receptors with excellent activity on a broad pest range, including Lepidoptera and Hemiptera. Herein we report on the synthesis, biological activity and mode-of-action for a class of 4-heterocyclic aryl isoxazoline insecticides.
