A series of novel 5,7-diphenylimidazo[1,2-a]pyridine derivatives was designed and synthesized. The in vitro cytotoxic activities of all the target compounds against human colorectal cancer(HT-29), human lung cancer(H460), human gastric cancer(MKN45) and human breast cancer(MDA-MB-231) cell lines were evaluated. The pharmacological results indicated that most of the target compounds showed moderate to excellent activities against the tested cell lines. The most promising compound 4h(0.20, 0.006, 0.08, 0.021 μmol/L) was 2.6, 5.1, 3.6 and 21.9 times more active than EPC2407(0.52, 0.031, 0.29, 0.46 μmol/L) against HT-29, H460, MKN45 and MDA-MB-231 cell lines, respectively.
| [1] |
MaZ Y, ZhangX H, LiC N, ZhengY J, YangG L, WangS K, HeYChem. Res. Chinese Universities, 2011, 275787
|
| [2] |
RebeccaS, DeepaN, AhmedinJCA Cancer J. Clin., 2013, 63: 11.
|
| [3] |
DowningK H, NogalesECurr. Opin. Cell Biol., 1998, 10: 16.
|
| [4] |
JordanM A, WilsonLNat. Rev. Cancer, 2004, 4: 253.
|
| [5] |
ShailajaK, HenrietteG, KarenM, JohnD, SanjeevaR, QiuL, ZhangH, FrederickB, DavidB, QuanY, JohnH, SergeL, CaiS XMol. Cancer Ther., 2004, 3: 1365
|
| [6] |
KamranM, RezaK, AlirezaF, AliM, HamidrezaM MMed. Chem. Res., 2011, 20: 920.
|
| [7] |
MajidM, JamshidD, MohammadR Z, AlirezaFBiomed. Pharmacother., 2011, 65: 175.
|
| [8] |
HassanA, MajidM, SeyedR M, MohammadR Z, AlirezaFArch. Pharm. Res., 2012, 35: 1573.
|
| [9] |
WilliamK, JohnD, JiangS C, ZhangH, WangY, ZhaoJ H, JiaS J, JohnH, DenisL, RichardS, KarenM, DavidB, RabindraR, RealD, CharlesB, SergeL, GiorgioA, HenrietteG, BenT, ShailajaK, CaiS XJ. Med. Chem., 2004, 47: 6299.
|
| [10] |
WilliamK, ShailajaK, JiangS C, ZhangH, ZhaoJ H, JiaS J, XuL F, CandaceC G, RealD, NancyB, LouisV, SylvieC, JenniferD, GiorgioA, DenisL, SergeL, HenrietteG, BenT, JohnD, CaiS XBioorg. Med. Chem. Lett., 2005, 15: 4745.
|
| [11] |
WuX Y, MaW, KiranG, GuoC HJ. Formos. Med. Assoc., 2013, 3: 115.
|
| [12] |
WilliamK, JohnD, JiangS C, ZhangH, ZhaoJ H, CandaceC G, XuL F, SergeL, HenrietteG, RealD, BenT, ShailajaK, CaiS XJ. Med. Chem., 2007, 50: 2858.
|
| [13] |
WilliamK, JohnD, JiangS C, ZhangH, CandaceC G, DenisL, MonicaB, GiorgioA, RealD, SergeL, HenrietteG, BenT, ShailajaK, CaiS XJ. Med. Chem., 2008, 51: 417.
|
| [14] |
WilliamK, JiangS C, WangY, ShailajaK, CandaceC G, MonicaB, DenisL, RealD, SergeL, GiorgioA, HenrietteG, BenT, JohnD, CaiS XBioorg. Med. Chem. Lett., 2008, 18: 603.
|
| [15] |
CaiS X, JohnD, WilliamKAnticancer Agents Med. Chem., 2009, 9: 437.
|
| [16] |
AlanR K, XuY J, TuH BJ. Org. Chem., 2003, 68: 4935.
|
| [17] |
CarolineC, MaximeD C, PatriceVHeterocycles, 2005, 65: 2979.
|
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Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH
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