62486-02-6Relevant articles and documents
Palladium-catalyzed α-arylation of indolin-3-ones
Chang, Yu-Hsuan,Chen, I-Chia,Hsu, Hsin-Yun,Peng, Wan-Ling,Wu, Yen-Ku
supporting information, p. 4660 - 4663 (2020/05/22)
A method for the catalytic α-arylation of indolin-3-ones was developed. The catalytic system comprising Pd(dba)2 and PAd3 was found to be optimal for the transformation. The protocol features broad functional group compatibility in that a range of arylated indoxyl derivatives bearing a fully substituted carbon center was synthesized with high efficiency. A preliminary bioassay study revealed that the selected indole-substituted indolin-3-ones exhibit favorable cytotoxic activities against HCT-116 cancer cell line.
Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands
Nirogia, Ramakrishna V.S.,Kambhampati, Ramasastri,Daulatabad, Anand V.,Gudla, Parandhama,Shaikh, Mohammad,Achanta, Pramod Kumar,Shinde, Anil K.,Dubey, Pramod Kumar
, p. 341 - 349 (2012/01/06)
A series of novel conformationally restricted N1-arylsulfonyl-3-aminoalkoxy indoles were designed and synthesized as 5-HT6 receptor (5-HT6R) ligands. Many of the synthesized compounds have moderate in vitro-binding affinities at 5-HT6R. The lead compound 8b (% inhibition=97.2 at 1 μM) from this series has good pharmacokinetic profile in male Wister rats and is active in animal model of cognition like Morris water maze. The details of chemistry, SAR, pharmacokinetics and pharmacological data constitute the subject matter of this report.