Novel Targeted Therapeutics for Castration Resistant Prostate Cancer
Technical Report,01 Sep 2018,31 Aug 2019
University of North Dakota Grand Forks United States
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Successful synthesis and purification of 5F02 analogs with different chemical properties. The effect of histone-dependent PARP-1 inhibitors on androgen-dependent and -independent activation of AR signaling was evaluated. The functional antitumor activity of 5F02 and its analogs was examined in androgen-dependent and castration-resistant PC cells. 5F02 and its analogs demonstrated superior antitumor activity compared with NAD-like clinically relevant PARP-1 inhibitors olaparib, veliparib, and rucaparib. Physicochemical and ADME properties of 5F02 and its analogs were examined.
- Medicine and Medical Research