432503-80-5Relevant academic research and scientific papers
Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents
Kawada, Hatsuo,Ebiike, Hirosato,Tsukazaki, Masao,Yamamoto, Shun,Koyama, Kohei,Nakamura, Mitsuaki,Morikami, Kenji,Yoshinari, Kiyoshi,Yoshida, Miyuki,Ogawa, Kotaro,Shimma, Nobuo,Tsukuda, Takuo,Ohwada, Jun
, p. 2897 - 2906 (2016)
Phosphoinositide 3-kinase (PI3K) is a promising anti-cancer target, because various mutations and amplifications are observed in human tumors isolated from cancer patients. Our dihydropyrrolopyrimidine derivative with a phenylurea moiety showed strong PI3
Novel and potent 5-piperazinyl methyl- N1-aryl sulfonyl indole derivatives as 5-HT6 receptor ligands
Nirogi, Ramakrishna V. S.,Kothmirkar, Prabhakar,Kambhampati, Ramasastri,Konda, Jagadish Babu,Arepalli, Sobhanadri,Pamuleti, Narasimhareddy G.,Deshpande, Amol D.,Bandyala, Trinathreddy,Shinde, Anil K.,Dubey
scheme or table, p. 340 - 344 (2010/11/18)
The exclusive distribution of 5-HT6 receptors in the brain regions associated with learning and memory makes it an ideal target for cognitive disorders. A novel series of 5-piperazinyl methyl-N1-aryl sulfonyl indoles were designed and synthesized as 5-HT6R ligands. Most of the synthesized compounds are potent when tested by in vitro radioligand binding assay. The lead compound from the series does not have the CYP liabilities and is active in an animal model of cognition.
