Design and synthesis of a novel class of furan-based molecules as potential 20S proteasome inhibitors.
A novel class of furan-based compounds as potential 20S proteasome inhibitors have been designed and synthesized, among which nine compounds are peptide derivatives and six molecules are statine peptidomimetics. The C-terminal furanyl moiety was introduced to target molecules as furan-based amino acids. All the compounds were obtained steadily with moderate to high yield. Compound 12 was a selective moderate potent proteasome peptidomimetic inhibitor. It inhibited HepG2 and HL-60 proliferation effectively.
Fu
Yiqiu
Y
Department of Medicinal Chemistry, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China.
Xu
Bo
B
Zou
Xiaomin
X
Ma
Chao
C
Yang
Xiaoming
X
Mou
Ke
K
Fu
Gang
G
Lü
Yang
Y
Xu
Ping
P
D000596:Amino Acids / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002918:Chymotrypsin / Q000737:chemistry; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005663:Furans / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008958:Models, Molecular; D061988:Proteasome Inhibitors
D000596:Amino Acids; D000970:Antineoplastic Agents; D005663:Furans; D061988:Proteasome Inhibitors; D002918:Chymotrypsin