Derivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one (1) demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects of (i) the heterocyclic ring, (ii) the alkoxy group at position 5 of the benzoxathiole ring, and (iii) the substituents in the phenyl ring B. Replacement of the sulfur atom by oxygen does not influence the activity. None of the listed structural fragments alone assured high cytotoxic activity.
Authors
- Marek T. Konieczny,
- Anita Bułakowska,
- Justyna Polak,
- Danuta Pirska,
- Wojciech Konieczny,
- Patrycja Gryń,
- prof. dr hab. inż. Andrzej Składanowski link open in new tab ,
- Michał Sabisz link open in new tab ,
- Krzysztof Lemke,
- Anna Pieczykolan,
- Marlena Gałązka,
- Katarzyna Wiciejowska,
- Joanna Wietrzyk
Additional information
- DOI
- Digital Object Identifier link open in new tab 10.1111/cbdd.12296
- Category
- Publikacja w czasopiśmie
- Type
- artykuł w czasopiśmie wyróżnionym w JCR
- Language
- angielski
- Publication year
- 2014
