Volume 1, Issue 1, April 2013, Page: 1-6
Green and Efficient Synthesis of Some Pyrido[2,3-D]Pyrimidin-4(3h)-One Derivatives Via Iodine Catalyst in Aqueous Media and Evaluation the Synthesized Compounds as Anticancer
Ayman M. F. Elgohary, Department of medical laboratories College of Applied Medical Science, Majmaah University, Almajma’ah 11952, KSA
E. M. Ezz El-Arab, National Organization For Drug Control & Research, Pharmaceutical Chemistry Division, Giza, Egypt
Received: Mar. 16, 2013;       Published: Apr. 2, 2013
DOI: 10.11648/j.sjc.20130101.11      View  3638      Downloads  245
Abstract
A series of new 2-propylpyrido[2,3-d]pyrimidin-4(3H)-one with different substituents at position 3 were syn-thesized by traditional method and Iodine catalyst method. The effect of the newly synthesized compounds was tested as anti-cancer in National Cancer Institute(NCI)in USA. Some of the synthesized compounds exploited potent antitumor activity, especially the compounds pyrido[2,3-d][1,3]oxazin (2), 3-amino derivative 3a, 3b and hydroxy derivative 3c dis-played the highest activity among the test compounds with IC50 > 5 mg/mL
Keywords
Pyrido[2,3-D][1,3]Oxazin-4-One, 2-Propylpyrido[2,3-D]Pyrimidin-4(3h)-One, Antitumor
To cite this article
Ayman M. F. Elgohary, E. M. Ezz El-Arab, Green and Efficient Synthesis of Some Pyrido[2,3-D]Pyrimidin-4(3h)-One Derivatives Via Iodine Catalyst in Aqueous Media and Evaluation the Synthesized Compounds as Anticancer, Science Journal of Chemistry. Vol. 1, No. 1, 2013, pp. 1-6. doi: 10.11648/j.sjc.20130101.11
Reference
[1]
S.N. VanderWel, P.J. Harvey, D.J. McNamara, J.T. Repine, P.R. Keller, J. Quin III, R.J. Booth, W.L. Elliott, E.M. Dobrusin, D.W. Fry, P.L. Toogood, J. Med. Chem 48 (2005) 2371e2378.
[2]
P.L. Toogood, P.J. Harvey, J.T. Repine, D.J. Sheehan, S.N. VanderWel, H. Zhou, P.R. Keller, D.J. McNamara, D. Sherry, T. Zhu, J. Brodfuehrer, C. Choi, M.R. Barvian, D.W. Fry, J. Med. Chem 48 (2005) 2388e2406.
[3]
B.D. Palmer, J.B. Smaill, G.W. Rewcastle, E.M. Dobrusin, A. Kraker, C.W. Moore, R.W. Steinkampf, W.A. Denny, Bioorg. Med.
[4]
K. Malagu, H. Duggan, K. Menear, M. Hummersone, S. Gomez, C. Bailey, P. Edwards, J. Drzewiecki, F. Leroux, M.J. Quesada, G. Hermann, S. Maine, C. Molyneaux, A. Le Gall, J. Pullen, I. Hickson, L. Smith, S. Maguire, N. Martin, G. Smith, M. Pass, Bioorg. Med. Chem. Lett. 19 (2009) 5950e5953.
[5]
X.L. Zhao, Y.F. Zhao, S.C. Guo, H.S. Song, D. Wang, P. Gong, Molecules 12 (2007) 1136e1146.
[6]
H.N. Hafez, A.B.A. El-Gazzar, Bioorg. Med. Chem. Lett. 19 (2009) 4143e4147.
[7]
A.S. Shawali, S.M. Sherif, M.A.A. Darwish, M.M. El-merzabani, Arch. Pharm. Res. 33 (2010) 55e60.
[8]
(a) Masuda, Satoru et al. Jpn.Kokai. Tokkyo Koho Jp 03, 106, 880. C.A.15: 183361d. (b) Tamura et al. Jpn. Kokai. Tokkyo Koho Jp 61, 249, 983, C.A. 106: 213979.
[9]
J. Ram, D.A. Vanden Berghe, A.J.J. Vlietinck, Heterocycl. Chem. 28 (1988) 217.
[10]
J.R. Piper, G.S. Mc Calab, J.A. Montgomery, R.L. Kishiuk, Y. Gamount, F.M. Sirotnak, J. Med. Chem. 29 (1986) 1080e1087.
[11]
R.K. Robins, G.H.J. Hitchings, Am. Chem. Soc. 80 (1958) 3449.
[12]
M.F. Hasan, A.M. Madkour, I. Saleem, J.M.A. Rahman, E.A.Z. Mohammed, Heterocycles 38 (1994) 57.
[13]
John Adams Lowe,Chem. Abstr. 112 (1990) 21008 Austrian At. 388378 (1989) 378.
[14]
A. Gangjee, O.O. Adair, S.F. Queener, J. Med. Chem. 46 (2003) 5074e5082. H. Iwamura, S. Murakami, K. Koshimizu, S. Matsabura, J. Med. Chem. 28 (1985)577e583.
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