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Dao, Viet Hung; Ourliac-Garnier, Isabelle; Logé, Cédric; McCarthy, Florence O; Bach, Stéphane; da Silva, Teresinha Gonçalves; Denevault-Sabourin, Caroline; Thiéfaine, Jérôme; Baratte, Blandine; Robert, Thomas; Gouilleux, Fabrice; Brachet-Botineau, Marie; Bazin, Marc-Antoine; Marchand, Pascal
Molecules (Basel, Switzerland), 10/2021, Letnik: 26, Številka: 21Journal Article
Pim kinases (proviral integration site for Moloney murine leukemia virus kinases) are overexpressed in various types of hematological malignancies and solid carcinomas, and promote cell proliferation and survival. Thus, Pim kinases are validated as targets for antitumor therapy. In this context, our combined efforts in natural product-inspired library generation and screening furnished very promising dibenzo , furan derivatives derived from cercosporamide. Among them, lead compound was highlighted as a potent Pim-1/2 kinases inhibitor with an additional nanomolar IC value against CLK1 (cdc2-like kinases 1) and displayed a low micromolar anticancer potency towards the MV4-11 (AML) cell line, expressing high endogenous levels of Pim-1/2 kinases. The design, synthesis, structure-activity relationship, and docking studies are reported herein and supported by enzyme, cellular assays, and larvae testing for acute toxicity.
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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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