5154-02-9Relevant academic research and scientific papers
Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds
Roth, Joshua,Madoux, Franck,Hodder, Peter,Roush, William R.
, p. 2628 - 2632 (2008/12/21)
Three synthetic routes were developed for structure-activity relationship (SAR) studies of HTS-derived isoquinolinone inhibitor probes for the orphan nuclear receptor steroidogenic factor-1 (NR5A1). Among the new analogs reported herein, 31 and 32 have im
Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process
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, (2008/06/13)
The invention is selected, novel, and known analogs of isoquinolinones of the formula and pharmaceutically acceptable salts thereof; novel pharmaceutical compositions; and a method for enhancing the lethal effects for tumor cells to treatment having DNA damaging activity such as ionizing radiation or with chemotherapeutic agents.
Synthesis and Biological Activity of 4-(Diphenylmethyl)-α--1-piperazineethanol and Related Compounds
Sircar, Ila,Haleen, Steve J.,Burke, Sandra E.,Barth, Hubert
, p. 4442 - 4449 (2007/10/02)
A series of 4-(diphenylmethyl)-α--1-piperazineethanol and closely related compounds was synthesised and evaluated for cardiac and vascular activity in isolated perfused rat and guinea pig hearts.Compound 1 produced greater inotropic effects in rat hearts than in guinea pig hearts, a phenomenon which was also observed with the prototype agent DPI 201-106.Compound 15 produced an inotropic effect with one-tenth the potency of compound 1.Both compounds 1 and 15 demonstrated direct inotropic and vasodilatory effects when administered iv in anesthetized dogs, although the vasodilatory activity was more pronounced with compound 15 than 1 and DPI compound.Compound 1 lacks the CN moiety which is a key structural requirement in DPI for positive inotropic activity.The synthesis, in vitro, and in vivo evaluations of these agents, and comparative data with DPI-201-106 (compound 17) are reported.
