Unfortunately, none of these compounds were efficacious in cell culture.
Although third-generation P-gp inhibitors were significantly efficacious in vitro, these compounds are not used clinically because in vivo and preclinical studies indicated a lack of efficacy and/or significant adverse effects [ 46].
Thus, CSNAP highlighted compounds with known anti-proliferative properties and analogs of these compounds that may be more efficacious.
Collectively, these data support the current understanding that D3T is the most efficacious of the three compounds, with the observed efficacies of D3T ⋙ TBD ≥ OLT.
The selectivity profile of these compounds provides great improvement over the commercial drug tamsulosin, hence may pave the way to the development of new and efficacious therapeutic agents with reduced side effects.
Megatons of these compounds are produced annually.
None of these compounds demonstrated selective cytotoxicity.
Interestingly, some of these compounds displayed different activation capabilities of the two receptor subtypes, as illustrated by TCBPA and chlordecone, which were significantly more efficacious for ERα (50% and 39%, respectively) than for ERβ (17%and19%9%, respectively).
However, our current results indicate that chronic, every other day treatment with CD, even when initiated post-weaning, proved significantly more beneficial than single [16], [19] or weekly injections of CD began at P7 and is the most efficacious of any compound tested to date in delaying NPC disease.
This observation, coupled with the structural flexibility revealed in the present study, suggests that isomeric iodinated analogues of celecoxib are efficacious COX-2 inhibitors, and these compounds can be efficiently labeled with [I] for use in COX-2-targeted SPECT imaging.
