Recommanded Product: 98-17-9. Pertusati, F; Ferla, S; Bassetto, M; Brancale, A; Khandil, S; Westwell, AD; McGuigan, C in [Pertusati, Fabrizio; Ferla, Salvatore; Bassetto, Marcella; Brancale, Andrea; Khandil, Sahar; Westwell, Andrew D.; McGuigan, Christopher] Sch Pharm & Pharmaceut Sci, Redwood Bldg,King Edwards 7 Ave, Cardiff CF10 3NB, S Glam, Wales published A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer in 2019, Cited 76. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.
SAR studies on bicalutamide, enobosarm and enzalutamide analogues, functionalised with polyfluorinated groups, is presented. Among the novel bicalutamide and enobosarm derivatives synthesised, several displayed significantly improved in vitro anticancer activity, with IC50 values in the low micromolar range against four different prostate cancer cell lines (LNCaP, VCaP, DU-145 and 22Rv1), showing up to 48-fold increase in comparison with the parent structures. In particular, SF5 enobosarm analogues were found to be most potent compounds, full AR antagonists and with favourable ADME properties. The most promising compound (48a) was evaluated for its in vivo efficacy in PC xenograft mouse model (22Rv1) with results comparable to the standard-of-care docetaxel. (C) 2019 Published by Elsevier Masson SAS.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles