Design, synthesis and SAR studies of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine as aminopeptidase N/CD13 inhibitors.
Aminopeptidase N (APN), belonged to metalloproteinase, is an essential peptidase involved in the process of tumor invasion and metastasis. A series of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine were designed, synthesized and evaluated for their ability to inhibit APN. Preliminary activity evaluation showed that most of target compounds possessed potent inhibitory activities against APN. With in this series, compound A6 and B6 exhibited good potency with the IC(50) values of 8.8+/-1.3 microM and 8.6+/-1.1 microM, respectively.
Shang
Luqing
L
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China.
Fang
Hao
H
Zhu
Huawei
H
Wang
Xuejian
X
Wang
Qiang
Q
Mu
Jiajia
J
Wang
Binghe
B
Kishioka
Shiroh
S
Xu
Wenfang
W
D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D003198:Computer Simulation; D003959:Diamines / Q000737:chemistry*; D015195:Drug Design; D018922:HL-60 Cells; D006801:Humans; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
C541071:3-phenylpropane-1,2-diamine; D003959:Diamines; D010455:Peptides; D011480:Protease Inhibitors; D018826:CD13 Antigens