162648-46-6Relevant articles and documents
INHIBITORS OF ENL/AF9 YEATS
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Paragraph 00137; 00139, (2021/06/26)
Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.
FUSED 1,4-DIHYDRODIOXIN DERIVATIVES AS INHIBITORS OF HEAT SHOCK TRANSCRIPTION FACTOR 1
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, (2015/04/22)
The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models
Szczepankiewicz,Chiou,Credo,Alder,Nukkala,Zielinski,Jarvis,Mollison,Frost,Bauch,Hui,Liu,Claiborne,Li,Rosenberg,Jae,Tasker,Gunawardana,Von Geldern,Gwaltney II,Wu-Wong,Gehrke
, p. 4416 - 4430 (2007/10/03)
During a screen for compounds that could inhibit cell proliferation, a series of new tubulin-binding compounds was identified with the discovery of oxadiazoline 1 (A-105972). This compound showed good cytotoxic activity against non-multi-drug-resistant and multi-drug-resistant cancer cell lines, but its utility in vivo was limited by a short half-life. Medicinal chemistry efforts led to the discovery of indolyloxazoline 22g (A-259745), which maintained all of the in vitro activity seen with oxadiazoline 1, but also demonstrated a better pharmacokinetic profile, and dose-dependent in vivo activity. Over a 28 day study, indolyloxazoline 22g increased the life span of tumor-implanted mice by up to a factor of 3 upon oral dosing. This compound, and others of its structural class, may prove to be useful in the development of new chemotherapeutic agents to treat human cancers.
Heterocyclic esters of rapamycin
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, (2008/06/13)
A compound of the structure STR1 wherein R and R1 are each, independently, STR2 or hydrogen, R2 is a heterocyclic radical which may be optionally substituted; n=0-6; with the proviso that R and R1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.