29202-13-9Relevant articles and documents
Design of a Tris-Heteroleptic Ru(II) Complex with Red-Light Excitation and Remarkably Improved Photobiological Activity
Gou, Shaohua,Li, Shuang,Wang, Xinyi,Xu, Gang,Zhao, Jian,Zhao, Qiang
, (2020)
Ru(II)-polypyridyl complexes are of increasing interest in photodynamic therapy (PDT) due to their easily tunable photophysical and photochemical properties. However, short-wavelength absorption of Ru(II)-polypyridyl complexes has limited their penetration depth in PDT. Herein, the series of Ru(II)-polypyridyl complexes 1-4 was designed by replacing one bipyridine in [Ru(bpy)3]Cl2 with Schiff bases (iminopyridine or iminoquinoline analogues) to achieve red-shifted absorption of Ru(II)-polypyridyl photosensitizers. To further shift the absorption to longer wavelength and improve the photobiological activity of Ru(II)-polypyridyl complexes, the three tris-heteroleptic Ru(II) complexes 5-7 with benzo[i]dipyrido[3,2-a:2′,3′-c]phenazine (dppn) as a ligand were designed to achieve long-lived intraligand (3IL) excited states. Cytotoxicity data against A549 and HepG2 cells revealed that complex 7 showed extraordinarily high cytotoxicity under 650 nm irradiation, resulting in IC50 values of 56 and 63 nM with exceptionally large phototoxicity index (PI) values of 763 and 613, respectively. Thus, the resulting complex 7 with considerable red-light photocytotoxicity and high PI values shows a promising potential for therapeutic applications, which represents a new scaffold of Ru(II)-polypyridyl photosensitizers for PDT in the therapeutic window . This study delivers a rational strategy for the design of tris-heteroleptic Ru(II) complexes as promising photosensitizers for cancer therapy. ?
Targeting metal-Aβ aggregates with bifunctional radioligand [11C]L2-b and a fluorine-18 analogue [18F]FL2-b
Cary, Brian P.,Brooks, Allen F.,Fawaz, Maria V.,Shao, Xia,Desmond, Timothy J.,Carpenter, Garrett M.,Sherman, Phillip,Quesada, Carole A.,Albin, Roger L.,Scott, Peter J. H.
, p. 112 - 116 (2015/03/04)
Interest in quantifying metal-Aβ species in vivo led to the synthesis and evaluation of [11C]L2-b and [18F]FL2-b as radiopharmaceuticals for studying the metallobiology of Alzheimer's disease (AD) using positron emission tomography (PET) imaging. [11C]L2-b was synthesized in 3.6% radiochemical yield (nondecay corrected, n = 3), >95% radiochemical purity, from the corresponding desmethyl precursor. [18F]FL2-b was synthesized in 1.0% radiochemical yield (nondecay corrected, n = 3), >99% radiochemical purity, from a 6-chloro pyridine precursor. Autoradiography experiments with AD positive and healthy control brain samples were used to determine the specificity of binding for the radioligands compared to [11C]PiB, a known imaging agent for β-amyloid (Aβ) aggregates. The Kd for [11C]L2-b and [18F]FL2-b were found to be 3.5 and 9.4 nM, respectively, from those tissue studies. Displacement studies of [11C]L2-b and [18F]FL2-b with PiB and AV-45 determined that L2-b binds to Aβ aggregates differently from known radiopharmaceuticals. Finally, brain uptake of [11C]L2-b was examined through microPET imaging in healthy rhesus macaque, which revealed a maximum uptake at 2.5 min (peak SUV = 2.0) followed by rapid egress (n = 2).
COMPOSITIONS AND METHODS FOR THE TREATMENT AND ANALYSIS OF NEUROLOGICAL DISORDERS
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Page/Page column 25-26, (2013/06/27)
Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-β (Aβ ) or metal-Aβ species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
