@article{4f5feada8a88472a946a07029e8b4ddb,
title = "Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin",
abstract = "A series of hybrid compounds of bestatin (1) and actinonin (3), which promote degradation of cellular inhibitor of apoptosis protein 1 (cIAP1), were designed and synthesized. Structure-activity relationship studies indicated that absolute configuration, hydrophobicity at the α-position of the internal amide carbonyl group, and the presence of a small substituent at the α-position of the ester group are important factors for the expression of potent cIAP1 degradation-promoting activity. HAB-5A (30b) showed the most potent activity (IC50 = 0.53 μM) among the compounds prepared.",
keywords = "Actinonin, Bestatin, Inhibitor, Structural development, cIAP1",
author = "Shinichi Sato and Masashi Tetsuhashi and Keiko Sekine and Hiroyuki Miyachi and Mikihiko Naito and Yuichi Hashimoto and Hiroshi Aoyama",
note = "Funding Information: The authors are grateful to Prof. Aya Tanatani (Ochanomizu University) for her helpful discussion. The work described in this paper was partially supported by Grants-in-Aid for Scientific Research from The Ministry of Education, Culture, Sports, Science and Technology, Japan, and the Japan Society for the promotion of Science.",
year = "2008",
month = apr,
day = "15",
doi = "10.1016/j.bmc.2008.02.024",
language = "English",
volume = "16",
pages = "4685--4698",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Limited",
number = "8",
}