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Isaac Hoffman

Explore the profile of Isaac Hoffman including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 11
Citations 59
Followers 0
Related Specialties
Chemistry
Biochemistry
Neurology
Top 10 Co-Authors
Robert Skene
Junya Shirai
Satoshi Yamamoto
Hideyuki Nakagawa
Mitsunori Kono
Ayumu Sato
Masaharu Nakayama
Atsuko Ochida
Yoshihide Tomata
Yoshiyuki Fukase
Published In
Bioorg Med Chem Lett
Bioorg Med Chem
J Med Chem
ChemMedChem
Neurochem Res
Affiliations
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Recent Articles
1.
Fatigue crack propagation and fracture toughness of cortical bone are radiation dose-dependent
Crocker D, Hoffman I, Carter J, Akkus O, Rimnac C
J Orthop Res . 2022 Aug; 41(4):823-833. PMID: 35949192
Cortical bone allograft sterilized with a standard γ-radiation dose of 25-35kGy has demonstrated reduced static and cyclic fracture resistance compared with unirradiated bone. To mitigate radiation damage, we recently observed...
2.
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors
Sasaki Y, Tokuhara H, Ohba Y, Okabe A, Nakayama M, Nakagawa H, et al.
Bioorg Med Chem Lett . 2020 Jan; 30(5):126963. PMID: 31980341
Herein we report an efficient method for the synthesis of a highly functionalized 2-pyrrolidinone, tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylate, from readily available starting materials. Utility of this compound was demonstrated in the synthesis...
3.
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent
Kurasawa O, Miyazaki T, Homma M, Oguro Y, Imada T, Uchiyama N, et al.
J Med Chem . 2020 Jan; 63(3):1084-1104. PMID: 31895562
In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported thieno[3,2-]pyrimidinone analogue showing time-dependent Cdc7 kinase inhibition and slow...
4.
Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists
Sato A, Fukase Y, Kono M, Ochida A, Oda T, Sasaki Y, et al.
ChemMedChem . 2019 Oct; 14(22):1917-1932. PMID: 31659845
Retinoic-acid-related orphan receptor γt (RORγt) inverse agonists could be used for the treatment of autoimmune diseases. Previously, we reported a novel quinazolinedione 1 a with a flexible linear linker as...
5.
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist
Yukawa T, Nara Y, Kono M, Sato A, Oda T, Takagi T, et al.
J Med Chem . 2019 Jan; 62(3):1167-1179. PMID: 30652849
Retinoic acid receptor-related orphan receptor γt (RORγt) agonists are expected to provide a novel class of immune-activating anticancer drugs via activation of Th17 cells and Tc17 cells. Herein, we describe...
6.
Identification of novel quinazolinedione derivatives as RORγt inverse agonist
Fukase Y, Sato A, Tomata Y, Ochida A, Kono M, Yonemori K, et al.
Bioorg Med Chem . 2018 Jan; 26(3):721-736. PMID: 29342416
Novel small molecules were synthesized and evaluated as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists for the treatment of inflammatory and autoimmune diseases. A hit compound, 1, was...
7.
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds
Shirai J, Tomata Y, Kono M, Ochida A, Fukase Y, Sato A, et al.
Bioorg Med Chem . 2017 Dec; 26(2):483-500. PMID: 29262987
A series of novel phenylglycinamides as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists were discovered through optimization of a high-throughput screen hit 1. (R)-N-(2-((3,5-Difluoro-4-(trimethylsilyl)phenyl) amino)-1-(4-methoxyphenyl)-2-oxoethyl)-3-hydroxy-N-methylisoxazole-5-carboxamide (22) was identified...
8.
Assessment of the Target Engagement and D-Serine Biomarker Profiles of the D-Amino Acid Oxidase Inhibitors Sodium Benzoate and PGM030756
Howley E, Bestwick M, Fradley R, Harrison H, Leveridge M, Okada K, et al.
Neurochem Res . 2017 Aug; 42(11):3279-3288. PMID: 28780732
Irregular N-methyl-D-aspartate receptor (NMDAR) function is one of the main hypotheses employed to facilitate understanding of the underlying disease state of schizophrenia. Although direct agonism of the NMDAR has not...
9.
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones
Kurasawa O, Oguro Y, Miyazaki T, Homma M, Mori K, Iwai K, et al.
Bioorg Med Chem . 2017 Mar; 25(7):2133-2147. PMID: 28284870
Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic study indicates that Cdc7 inhibition can induce selective...
10.
Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate
Keung W, Boloor A, Brown J, Kiryanov A, Gangloff A, Lawson J, et al.
Bioorg Med Chem Lett . 2017 Jan; 27(4):1099-1104. PMID: 28082036
Axl has been a target of interest in the oncology field for several years based on its role in various oncogenic processes. To date, no wild-type Axl crystal structure has...