Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N'-substituted-2,6-piperidinedione.
Aminopeptidase N (APN/CD13) over expressed on tumor cells, plays a critical role in tumor invasion, metastasis, and tumor angiogenesis. Here we described the design, synthesis and preliminary activity studies of novel APN inhibitors with 3-phenylalanyl-N'-substituted-2,6-piperidinedione scaffold. The results showed that compound 7c had the most potent inhibitory activity against APN with the IC(50) value to 5.00 +/-3.17 microM, which could be used as the lead compound in the future for anticancer agent research.
Zhang
Xiaopan
X
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, PR China.
Fang
Hao
H
Zhu
Huawei
H
Wang
Xuejian
X
Zhang
Lei
L
Li
Minyong
M
Li
Qianbin
Q
Yuan
Yumei
Y
Xu
Wenfang
W
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D010649:Phenylalanine / Q000138:chemical synthesis / Q000737:chemistry; D010881:Piperidones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013552:Swine
D000970:Antineoplastic Agents; D010881:Piperidones; D011480:Protease Inhibitors; D010649:Phenylalanine; D018826:CD13 Antigens