Literature DB >> 19117758

Efficient synthesis and biological evaluation of 1,2,9-trisubstituted 1,9-dihydro-6H-purin-6-ones.

Nian-Yu Huang1, Yong-Ju Liang, Ming-Wu Ding, Li-Wu Fu, Hong-Wu He.   

Abstract

The carbodiimides 4, obtained from aza-Wittig reactions of iminophosphorane 3 with aromatic isocyanates, reacted with amines in the presence of a catalytic amount of RO(-)Na(+) to give the 1,2,9-trisubstituted 1,9-dihydro-6H-purin-6-ones 6 in good yields. Compound 6 exhibited cytotoxicity against various cancer cells. For example, compounds 6b showed the best inhibition activities against KB, HepG2 and OVCAR3 with IC(50) 9.5, 20.4 and 10.0 microM.

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Year:  2008        PMID: 19117758     DOI: 10.1016/j.bmcl.2008.12.007

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Ethyl 2-methyl-6-(propan-2-yl-amino)-4-sulfanyl-idene-3H,11H-pyrimido[1,6-c]quinazoline-1-carboxyl-ate.

Authors:  Hong-Xia Li; Yu-Su Song; Yong-Nian Qu; Jiang-Bing Lu; Hong-Mei Wang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-05-19

2.  7-Benzyl-3-(4-chloro-phen-yl)-2-isobutyl-amino-5,6,7,8-tetra-hydro-pyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one.

Authors:  Hong Chen; Quan-Bin Liao
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-02-24

3.  7-Benzyl-3-(4-fluoro-phen-yl)-2-(pyrrol-idin-1-yl)-5,6,7,8-tetra-hydro-pyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one.

Authors:  Hong Chen; Hai-Jun Hu; Kai Yan; Qiu-Hong Dai
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-08-02

4.  7-Benzyl-2-[(cyclo-propyl-meth-yl)amino]-3-phenyl-5,6,7,8-tetra-hydro-pyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one.

Authors:  Hong Chen
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-07-30

5.  6-Benzyl-2-[(triphenyl-λ-phosphanyl-idene)amino]-4,5,6,7-tetra-hydro-thieno[2,3-c]pyridine-3-carbonitrile.

Authors:  Hong Chen; Kai Yan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-09-03

6.  7-Benzyl-3-(4-fluoro-phen-yl)-2-propyl-amino-5,6,7,8-tetra-hydro-pyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one.

Authors:  Hai-Jun Hu; Hong Chen
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-17
  6 in total

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