Letourneau, J.J., Riviello, C.M., Li, H., Cole, A.G., Ho, K., Zonetakos, H.A., Desai, H., Zhao, J., Auld, D.S., Napier, S.E., Thomson, F.J., Goan, K.A., Morphy, J.R., Ohlmeyer, M.H.J. and Webb, M.L. (2010) Idendification and Optimi- zation of Novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide Vasopressin V3 (V1b) Receptor Antagonists. Bioorganic & Medicinal Chemistry Letters, 20, 5394-5397. http://dx.doi.org/10.1016/j.bmcl.2010.07.118

has been cited by the following article:

• TITLE: Utility of 2-Methyl-quinazolin-4(3H)-one in the Synthesis of Heterocyclic Compounds with Anticancer Activity

  AUTHORS: Aisha Youssif Hassan Helali, Marwa Taha Mostafa Sarg, Makarem Mohamed Said Koraa, Mona Said Fathy El-Zoghbi

  KEYWORDS: Quinazoline; Anticancer; DHFR; TS

  JOURNAL NAME: Open Journal of Medicinal Chemistry, Vol.4 No.1, March 27, 2014

  ABSTRACT: Quinolino[2,1-b]quinazolines 3 and 4, pyrrolo[2,1-b]quinazoline 5 and various substituted 2-(4-chlorostyryl)quinazoline derivatives including: 4-amino derivative 8, 4-hydrazino derivative 9, thiourea derivative 10, thiosemicarbazide derivative 19, 4-benzylidene hydrazinyl derivative 21, 4-amino thiazolidene derivatives 11, 12, 13, 22, imidazoquinazolines 15, 16, quinazolinium chloride 14, triazino[4,3-c]quinazolines 17, 18, tetrazino[1,6-c]quinazoline 20, 4-amino azetidinyl derivative 23, triazolo[4,3-c]quinazoline 24, 4-amino substituted quinazolines 25, 26, 27, 29 and quinazolino quinazoline 28 were synthesized through different chemical reactions. The obtained compounds were evaluated for their in vitro antitumor activity against HEPG2 and MCF-7 cell lines compared to the reference drug (doxorubicin). Compounds 18, 19, 20, 23 and 24 were found to be the most active against both cell lines exhibiting IC50 values ranging from 10.82 - 29.46 μM/L and 7.09 - 31.85 μM/L against Hep-G2 and MCF-7 cell lines, respectively, in addition to docking study of these five compounds against thymidylate synthase and dihydrofolate reductase enzymes active sites.