13078-91-6Relevant articles and documents
FUSED THIAZOLOPYRIMIDINE DERIVATIVES AS MNKS INHIBITORS
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Page/Page column 68; 69, (2017/06/12)
The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.
Nucleophilic substitution reaction of N-2-(1-hydroxyindol-3-yl)ethylindole-3-acetamide and -1-hydroxyindole-3-acetamide
Nakai, Yu-ya,Goto, Aya,Yamada, Fumio,Somei, Masanori
, p. 1589 - 1600 (2007/10/03)
Syntheses of N-2-(1-hydroxyindol-3-yl)ethyl-1-hydroxyindole-3-acetamide (3a) and -indole-3-acetamide (4a) are reported. They undergo nucleophilic substitution reaction at the 1-position upon reaction with indole in 85% formic acid to give new type compounds, N-2-[1-(indol-3-yl)indol-3-yl]ethylindole-3-acetamide (13), N-2-(indol-3-yl)ethyl-(14), and N-2-[1-(indol-3-yl)indol-3-yl]ethyl-1-(indol-3-yl)indole-3-acetamide (15).
Cardiac-Slowing Amidines Containing the 3-Thioindole Group. Potential Antianginal Agents
Zelesko, Michael J.,McComsey, David F.,Hageman, William E.,Nortey, Samuel O.,Baker, Carol A.,Maryanoff, Bruce E.
, p. 230 - 237 (2007/10/02)
A series of 3-thioindolamidines (and 3-indolamidines) related to mixidine (1) was studied for cardiac-slowing properties, allowing the discovery of activity for prototype thioindole 2.Structure-activity relationships were explored, leading to many potent antitachycardic agents (6-9, 12, 13, 15-17, 20, 23, 24, 30, 34, 35, 45, and 47-49).Relative to 2, cardiac-slowing activity is enhanced by substitution of the indole nitrogen with small (C1-C3) saturated alkyl groups (6-9), unsaturated alkyl groups (12, 13, and 15-17), or a methoxyethyl group (20); replacement of the N-methyl group with alkyl (23) or phenyl groups (24); and extension of the ethylene bridge by two methylene units (34).Dethio (i.e., 3-indole) analogues of 2 with alkyl substitution on the indole nitrogen (47-49) have greater activity as well.Several potent compounds were also found to have minimal myocardial depression (6-9, 13, 45, and 47).Secondary pharmacological testing is reported for thioindoles 2, 6, 7, 9, and 28.