Design and synthesis of 4-acetoxypentanamide derivatives of spliceostatin A and their biological evaluation towards prostate cancer treatment

• Published in: Bioorganic & medicinal chemistry letters Vol. 91; p. 129333
• Main Authors: Hirabayashi, Satoru, Tsuyuguchi, Yuko, Li, Yue, Ohta, Noriko, Yoshikawa, Yusuke, Lin, Bangzhong, Fumimoto, Megumi, Nunomura, Kazuto, Suzuki, Takeyuki, Haruta, Junichi, Nimura, Keisuke, Arisawa, Mitsuhiro
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.07.2023; Elsevier
• Subjects: Chemistry; Chemistry, Medicinal; Chemistry, Organic; Humans; Life Sciences & Biomedicine; Male; Michael acceptor; Pharmacology & Pharmacy; Physical Sciences; Prostate cancer; Prostatic Neoplasms - drug therapy; Protein Isoforms; Pyrans; Receptors, Androgen; Science & Technology; Spiro Compounds; Spliceostatin A; Splicing variant; SSA; SF3B2; AR-V7; TBS; Michael acceptor; DIPEA; Et3N; Splicing variant; TFA; LHMDS; AR; TBAF; Spliceostatin A; DMAP; HATU; CRPC; KHMDS; Prostate cancer; ENZALUTAMIDE

[Display omitted] We designed and synthesized novel 4-acetoxypentanamide derivatives of spliceostatin A, whose 4-acetoxypentenamide moiety is reduced (7), isomerized (8), or substituted with methyl at the α-position (9). The results of biological evaluation against AR-V7 and the docking analysis of...