Title : Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines - Ansari_2008_Bioorg.Med.Chem_16_7691 |
Author(s) : Ansari FL , Iftikhar F , Ihsan Ul H , Mirza B , Baseer M , Rashid U |
Ref : Bioorganic & Medicinal Chemistry , 16 :7691 , 2008 |
Abstract :
Solid-phase synthesis of a parallel library of 3'-hydroxy-2,3-dihydrobenzothiazepines has been carried out through [4+3] annulation of alpha,beta-unsaturated ketones with aminothiophenol, using Wang resin as solid support. The synthesized compounds were evaluated for their potential as antibacterial, tumor inhibitors as well as acetyl- and butyrylcholinesterase inhibitors. None of the compounds showed any significant antibacterial activity. However, quite a few compounds showed significant potential as crown gall tumor inhibitors. These results reflect a strong exploratory potential in search of new benzothiazepines as source of anticancer agents. The results of the inhibition of cholinesterase revealed that benzothiazepines have a greater potential as butyrylcholinesterase inhibitors as compared to acetylcholinesterase. Moreover, the substitution of hydroxy group at C-3 in ring A led to increased activity when compared to unsubstituted- and 2'-OH substituted benzothiazepines. |
PubMedSearch : Ansari_2008_Bioorg.Med.Chem_16_7691 |
PubMedID: 18650096 |
Ansari FL, Iftikhar F, Ihsan Ul H, Mirza B, Baseer M, Rashid U (2008)
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines
Bioorganic & Medicinal Chemistry
16 :7691
Ansari FL, Iftikhar F, Ihsan Ul H, Mirza B, Baseer M, Rashid U (2008)
Bioorganic & Medicinal Chemistry
16 :7691