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Tria, George S; Abrams, Tinya; Baird, Jason; Burks, Heather E; Firestone, Brant; Gaither, L Alex; Hamann, Lawrence G; He, Guo; Kirby, Christina A; Kim, Sunkyu; Lombardo, Franco; Macchi, Kaitlin J; McDonnell, Donald P; Mishina, Yuji; Norris, John D; Nunez, Jill; Springer, Clayton; Sun, Yingchuan; Thomsen, Noel M; Wang, Chunrong; Wang, Jianling; Yu, Bing; Tiong-Yip, Choi-Lai; Peukert, Stefan
Journal of medicinal chemistry, 04/2018, Letnik: 61, Številka: 7Journal Article
In breast cancer, estrogen receptor alpha (ERα) positive cancer accounts for approximately 74% of all diagnoses, and in these settings, it is a primary driver of cell proliferation. Treatment of ERα positive breast cancer has long relied on endocrine therapies such as selective estrogen receptor modulators, aromatase inhibitors, and selective estrogen receptor degraders (SERDs). The steroid-based anti-estrogen fulvestrant (5), the only approved SERD, is effective in patients who have not previously been treated with endocrine therapy as well as in patients who have progressed after receiving other endocrine therapies. Its efficacy, however, may be limited due to its poor physicochemical properties. We describe the design and synthesis of a series of potent benzothiophene-containing compounds that exhibit oral bioavailability and preclinical activity as SERDs. This article culminates in the identification of LSZ102 (10), a compound in clinical development for the treatment of ERα positive breast cancer.
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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.
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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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