Abstract
The diastereoselective access to highly functionalized cyclopenta[c ]thiophene derivatives, potential useful scaffolds in medicinal chemistry, is described
starting from aminocyclopenta[c ]thiophenones.
Key words
stereoselective synthesis - cyclopenta[c ]thiophene - diastereoselectivity - Mitsunobu reaction - halogenation
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The cytotoxic activity of test compounds was evaluated in the NCI’s (National Cancer
Institute, Bethesda, USA) in vitro human disease-oriented antitumor screen. This screening
panel consists of 60 human tumor cell lines. Nine subpanels represent diverse histologies,
i.e. nonsmall cell lung, renal, breast cancers, central nervous system, colon, melanoma,
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at 10-fold dilutions. Results are evaluated in terms of specificity and potency. The
cytotoxic effects of each compounds are expressed as the molar drug concentration
required for 50% growth inhibition (GI50 ), total growth inhibition (TGI), and 50% cell kill (LC50 ).
