372198-41-9Relevant articles and documents
Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent
Brachet, Etienne,Dumond, Aurore,Liu, Wang-Qing,Fabre, Marie,Selkti, Mohamed,Raynaud, Fran?oise,Hermine, Olivier,Benhida, Rachid,Belmont, Philippe,Garbay, Christiane,Lepelletier, Yves,Ronco, Cyril,Pagès, Gilles,Demange, Luc
supporting information, (2019/11/21)
We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The p
Inhibitors of Neuropilin and use thereof for the treatment of Neuropilin-related diseases
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Paragraph 0119; 0120, (2015/02/02)
The present invention relates to a compound of general formula (I), and salts or solvate thereof, for treating a Neuropilin-related disease, disorder or condition; and to a composition, a pharmaceutical composition and a medicament comprising the compound of general formula (I).
INHIBITOR OF NEUROPILIN AND USE THEREOF FOR THE TREATMENT OF NEUROPILIN-RELATED DISEASES
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Page/Page column 34, (2015/02/02)
The present invention relates to a compound of general formula (I), and salts or solvate thereof, for treating a Neuropilin-related disease, disorder or condition; and to a composition, a pharmaceutical composition and a medicament comprising the compound of general formula (I).
Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR
Kendall, Jackie D.,Giddens, Anna C.,Tsang, Kit Yee,Frédérick, Rapha?l,Marshall, Elaine S.,Singh, Ripudaman,Lill, Claire L.,Lee, Woo-Jeong,Kolekar, Sharada,Chao, Mindy,Malik, Alisha,Yu, Shuqiao,Chaussade, Claire,Buchanan, Christina,Rewcastle, Gordon W.,Baguley, Bruce C.,Flanagan, Jack U.,Jamieson, Stephen M.F.,Denny, William A.,Shepherd, Peter R.
experimental part, p. 58 - 68 (2012/02/14)
Structure-activity relationship studies of the pyrazolo[1,5-a]pyridine class of PI3 kinase inhibitors show that substitution off the hydrazone nitrogen and replacement of the sulfonyl both gave a loss of p110α selectivity, with the exception of an N-hydroxyethyl analogue. Limited substitutions were tolerated around the phenyl ring; in particular the 2,5-substitution pattern was important for PI3 kinase activity. The N-hydroxyethyl compound also showed good inhibition of cell proliferation and inhibition of phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity. It had suitable pharmacokinetics for evaluation in vivo, and showed tumour growth inhibition in two human tumour cell lines in xenograft studies. This work has provided suggestions for the design of more soluble analogues.
PYRAZOLO[1,5-A]PYRIDINES AND THEIR USE IN CANCER THERAPY
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Page/Page column 76, (2009/03/07)
Pyrazolo[1,5-a]pyridines are described, including methods for their preparation, and their use as agents or drugs for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.