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. 2014 Jun 26;19(7):8916-32.
doi: 10.3390/molecules19078916.

Synthesis and evaluation of 2,4-disubstituted quinazoline derivatives with potent anti-angiogenesis activities

Guangjin Yu  1 , Zeng Li  2 , Liang Tang  3 , Qiru Xiong  4
Affiliations

Synthesis and evaluation of 2,4-disubstituted quinazoline derivatives with potent anti-angiogenesis activities

Guangjin Yu et al. Molecules. .

Abstract

A series of 2,4-disubstituted quinazoline derivatives were designed and synthesized. The biological results showed that most of quinazoline derivatives exhibited potent antiproliferative activities against a panel of three tumor cell lines and a good inhibitory effect against the adhesion and migration of human umbilical vein endothelial cells (HUVECs). Among these compounds, 11d was the most potent agent, that also exhibited the highest anti-angiogenesis activities in the chick embryo chorioallantoic membrane (CAM) assay.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Structure of ZD6474 and 2,4-disubstituted quinazoline derivatives.
Scheme 1
Scheme 1
Synthesis of quinazoline derivatives.
Figure 2
Figure 2
The inhibitory effects of quinazoline derivatives on HUVEC migration at doses of 15 μM and 30 μM.
Figure 3
Figure 3
The results of CAM assay. NaCl solution (0.9%) and thalidomide were used as a negative control and a positive control, respectively. Representative pictures of independent experiments performed in duplicate for the quinazoline derivatives 10d, 11a–d and 12d doses and controls. All filter discs had the same size, and any visual size differences are due to the various distances from which pictures were taken.
See this image and copyright information in PMC

References

    1. Grothey A., Galanis E. Targeting angiogenesis: Progress with anti-VEGF treatment with large molecules. Nat. Rev. Clin. Oncol. 2009;6:507–518. doi: 10.1038/nrclinonc.2009.110. - DOI - PubMed
    1. Folkman J. Tumor angiogenesis. Adv. Cancer Res. 1985;43:175–203. doi: 10.1016/S0065-230X(08)60946-X. - DOI - PubMed
    1. Ingber D., Fujita T., Kishimoto S., Sudo K., Kanamaru T., Brem H., Folkman J. Synthetic analogues of fumagillin that inhibit angiogenesis and suppress tumour growth. Nature. 1990;348:555–557. doi: 10.1038/348555a0. - DOI - PubMed
    1. Fong T.A., Shawver L.K., Sun L., Tang C., App H., Powell T.J., Kim Y.H., Schreck R., Wang X., Risau W., et al. SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types. Cancer Res. 1999;59:99–106. - PubMed
    1. O’Reilly M.S., Holmgren L., Shing Y., Chen C., Rosenthal R.A., Moses M., Lane W.S., Cao Y., Sage E.H., Folkman J. Angiostatin: A novel angiogenesis inhibitor that mediates the suppression of metastases by a Lewis lung carcinoma. Cell. 1994;79:315–328. doi: 10.1016/0092-8674(94)90200-3. - DOI - PubMed

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