Search Results - "Surti, Neha"
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The Discovery of Macrocyclic XIAP Antagonists from a DNA-Programmed Chemistry Library, and Their Optimization To Give Lead Compounds with in Vivo Antitumor Activity
Published in Journal of medicinal chemistry (26-03-2015)“…Affinity selection screening of macrocycle libraries derived from DNA-programmed chemistry identified XIAP BIR2 and BIR3 domain inhibitors that displace bound…”
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Discovery, Structure–Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2‑Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain
Published in Journal of medicinal chemistry (12-08-2021)“…Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an…”
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Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2‑Associated Kinase 1 Inhibitors
Published in Journal of medicinal chemistry (10-03-2022)“…Adaptor protein 2-associated kinase 1 (AAK1) is a serine/threonine kinase that was identified as a therapeutic target for the potential treatment of…”
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Conversion of carbazole carboxamide based reversible inhibitors of Bruton’s tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series
Published in Bioorganic & medicinal chemistry letters (01-10-2018)“…[Display omitted] •Electrophilic groups increased potency and selectivity of carbazole BTK inhibitors.•Related indole analogs retained this potency and further…”
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Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)
Published in Bioorganic & medicinal chemistry letters (01-10-2015)“…[Display omitted] Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton’s tyrosine kinase (BTK). 4,7- and…”
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Purine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors for autoimmune diseases
Published in Bioorganic & medicinal chemistry letters (01-05-2014)“…Investigation of various heterocyclic core isosteres of imidazopyrazines 1 &2 yielded purine derivatives 3 &8 as potent and selective BTK inhibitors…”
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Leveraging the IncuCyte Technology for Higher-Throughput and Automated Chemotaxis Assays for Target Validation and Compound Characterization
Published in SLAS discovery (01-02-2018)“…Chemotaxis is the directional movement of cells in response to a chemical stimulus and is vital for many physiological processes, including immune responses,…”
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Rapid Compound Integrity Assessment for High-Throughput Screening Hit Triaging
Published in SLAS discovery (01-02-2021)“…Hits from high-throughput screening (HTS) assays are typically evaluated using cheminformatics and/or empirical approaches before a decision for follow-up…”
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