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1.
Structure-activity relationship around PI-2620 highlights the importance of the nitrogen atom position in the tricyclic core.
Bioorg Med Chem
; 52: 116528, 2021 12 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-34839158
2.
Discovery and preclinical characterization of [18F]PI-2620, a next-generation tau PET tracer for the assessment of tau pathology in Alzheimer's disease and other tauopathies.
Eur J Nucl Med Mol Imaging
; 46(10): 2178-2189, 2019 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-31264169
3.
Discovery and characterization of novel indole and 7-azaindole derivatives as inhibitors of ß-amyloid-42 aggregation for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett
; 27(6): 1405-1411, 2017 03 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-28216401
4.
Synthesis and structure-activity relationship of 2,6-disubstituted pyridine derivatives as inhibitors of ß-amyloid-42 aggregation.
Bioorg Med Chem Lett
; 26(14): 3330-3335, 2016 07 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27256911
5.
Discovery and structure activity relationship of small molecule inhibitors of toxic ß-amyloid-42 fibril formation.
J Biol Chem
; 287(41): 34786-800, 2012 Oct 05.
Artículo
en Inglés
| MEDLINE | ID: mdl-22891248
6.
PI-2620 Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer's Disease and Other Tauopathies.
J Med Chem
; 64(17): 12808-12830, 2021 09 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-34455780
7.
Discovery of 2-(4-(2-fluoroethoxy)piperidin-1-yl)-9-methyl-9H-pyrrolo[2,3-b:4,5-c']dipyridine ([18F]PI-2014) as PET tracer for the detection of pathological aggregated tau in Alzheimer's disease and other tauopathies.
Eur J Med Chem
; 204: 112615, 2020 Oct 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-32771872
8.
Tau PET imaging with 18F-PI-2620 in Patients with Alzheimer Disease and Healthy Controls: A First-in-Humans Study.
J Nucl Med
; 61(6): 911-919, 2020 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-31712323
9.
Evaluation of Dosimetry, Quantitative Methods, and Test-Retest Variability of 18F-PI-2620 PET for the Assessment of Tau Deposits in the Human Brain.
J Nucl Med
; 61(6): 920-927, 2020 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-31712324
10.
3'-Intercalation of a N2-dG 1R-trans-anti-benzo[c]phenanthrene DNA adduct in an iterated (CG)3 repeat.
Chem Res Toxicol
; 21(7): 1348-58, 2008 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-18549249
11.
Translesion replication of benzo[a]pyrene and benzo[c]phenanthrene diol epoxide adducts of deoxyadenosine and deoxyguanosine by human DNA polymerase iota.
Nucleic Acids Res
; 30(23): 5284-92, 2002 Dec 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-12466554
12.
Ketones as building blocks for dynamic combinatorial libraries: highly active neuraminidase inhibitors generated via selection pressure of the biological target.
J Med Chem
; 46(3): 356-8, 2003 Jan 30.
Artículo
en Inglés
| MEDLINE | ID: mdl-12540234
13.
A new class of potent matrix metalloproteinase 13 inhibitors for potential treatment of osteoarthritis: Evidence of histologic and clinical efficacy without musculoskeletal toxicity in rat models.
Arthritis Rheum
; 60(7): 2008-18, 2009 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-19565489
14.
Error-prone translesion synthesis by human DNA polymerase eta on DNA-containing deoxyadenosine adducts of 7,8-dihydroxy-9,10-epoxy-7,8,9,10-tetrahydrobenzo[a]pyrene.
J Biol Chem
; 280(48): 39684-92, 2005 Dec 02.
Artículo
en Inglés
| MEDLINE | ID: mdl-16188888
15.
Benzo[a]pyrene-dG adduct interference illuminates the interface of vaccinia topoisomerase with the DNA minor groove.
J Biol Chem
; 278(11): 9905-11, 2003 Mar 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-12524450
16.
Inhibition of Werner syndrome helicase activity by benzo[c]phenanthrene diol epoxide dA adducts in DNA is both strand-and stereoisomer-dependent.
J Biol Chem
; 278(42): 41126-35, 2003 Oct 17.
Artículo
en Inglés
| MEDLINE | ID: mdl-12881525
17.
Site-specific DNA transesterification by vaccinia topoisomerase: effects of benzo[alpha]pyrene-dA, 8-oxoguanine, 8-oxoadenine and 2-aminopurine modifications.
J Biol Chem
; 278(43): 42170-7, 2003 Oct 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-12909623
18.
Different effects on human topoisomerase I by minor groove and intercalated deoxyguanosine adducts derived from two polycyclic aromatic hydrocarbon diol epoxides at or near a normal cleavage site.
J Biol Chem
; 277(16): 13666-72, 2002 Apr 19.
Artículo
en Inglés
| MEDLINE | ID: mdl-11832494
19.
Target-induced formation of neuraminidase inhibitors from in vitro virtual combinatorial libraries.
Proc Natl Acad Sci U S A
; 99(6): 3382-7, 2002 Mar 19.
Artículo
en Inglés
| MEDLINE | ID: mdl-11891312
20.
Position-specific trapping of topoisomerase II by benzo[a]pyrene diol epoxide adducts: implications for interactions with intercalating anticancer agents.
Proc Natl Acad Sci U S A
; 100(21): 12498-503, 2003 Oct 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-14523238