Abstract:
:Some new ethyl 2-[3-(4-unsubstituted or 4-substituted phenylsufonyl)ureido]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylates 3a-c, 2-[3-(phenylsulfonyl)ureido]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carbohydrazides 4a-f, 3-phenylsulfonyl-6,7,8,9-tetrahydro-5H-cyclohepta[1',2':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)dione 5 and 3-(phenylsulfonyl)-1-[3-(alkylaminocarbonyl or substituted piperazinylcarbonyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl]ureas 6a-d have been synthesized and tested for their antitumor activity. Among these compounds, 4a, 4c and 4d exhibited a broad spectrum antitumor activity with full panel (MG-MID) median growth inhibition (GI(50)) of 3.5, 4.9 and 4.0muM respectively. In addition, compounds 4c, 4d, 6c and 6d proved to be of moderate selectivity toward colon cancer cell lines with ratios of 3.1, 1.2, 3.6 and 3.0 respectively. Molecular modeling and pharmacophore prediction methods are used to study the antitumor activity of the most active compounds compared with the least active species by means of the molecular mechanic method.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
El-Sherbeny MA,Abdel-Aziz AA,Ahmed MAdoi
10.1016/j.ejmech.2009.11.014subject
Has Abstractpub_date
2010-02-01 00:00:00pages
689-97issue
2eissn
0223-5234issn
1768-3254pii
S0223-5234(09)00584-4journal_volume
45pub_type
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