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Pasqua, A. Elisa; Sharp, Swee Y.; Chessum, Nicola E. A.; Hayes, Angela; Pellegrino, Loredana; Tucker, Michael J.; Miah, Asadh; Wilding, Birgit; Evans, Lindsay E.; Rye, Carl S.; Mok, N. Yi; Liu, Manjuan; Henley, Alan T.; Gowan, Sharon; De Billy, Emmanuel; te Poele, Robert; Powers, Marissa; Eccles, Suzanne A.; Clarke, Paul A.; Raynaud, Florence I.; Workman, Paul; Jones, Keith; Cheeseman, Matthew D.
Journal of medicinal chemistry, 04/2023, Letnik: 66, Številka: 8Journal Article
CCT251236 1, a potent chemical probe, was previously developed from a cell-based phenotypic high-throughput screen (HTS) to discover inhibitors of transcription mediated by HSF1, a transcription factor that supports malignancy. Owing to its activity against models of refractory human ovarian cancer, 1 was progressed into lead optimization. The reduction of P-glycoprotein efflux became a focus of early compound optimization; central ring halogen substitution was demonstrated by matched molecular pair analysis to be an effective strategy to mitigate this liability. Further multiparameter optimization led to the design of the clinical candidate, CCT361814/NXP800 22, a potent and orally bioavailable fluorobisamide, which caused tumor regression in a human ovarian adenocarcinoma xenograft model with on-pathway biomarker modulation and a clean in vitro safety profile. Following its favorable dose prediction to human, 22 has now progressed to phase 1 clinical trial as a potential future treatment for refractory ovarian cancer and other malignancies.
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Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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