Abstract:
:3-(Alkyl(dialkyl)amino)benzothieno[2,3-f]quinazolin-1(2H)-ones (4-9) have been designed using Ellipticine structure as a model, replacing the carbazole core and the pyridine ring with a dibenzothiophene and a pyrimidine moiety, respectively. New benzothienoquinazolinones (4-9) have been synthesized by a simple one-pot reaction employing 3-aminodibenzothiophene as starting material. The benzothienoquinazolinones obtained (4-9), were evaluated for their anticancer activity against two breast cancer cell lines, MDA-MB-231 and MCF-7. The results revealed that compounds 4 and 7 presented a good antitumor activity toward the triple negative MDA-MB-231, without cytotoxicity against non-tumoral cells. Furthermore, the compounds 4 and 7 can be considered important molecular multi-target tools for their dual inhibition of different cellular proteins, i.e. Tubulin and human Topoisomerase I, involved in relevant cellular processes, as predicted by in silico studies and demonstrated by in vitro assays (for compound 4).
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Ceramella J,Caruso A,Occhiuzzi MA,Iacopetta D,Barbarossa A,Rizzuti B,Dallemagne P,Rault S,El-Kashef H,Saturnino C,Grande F,Sinicropi MSdoi
10.1016/j.ejmech.2019.111583subject
Has Abstractpub_date
2019-11-01 00:00:00pages
111583eissn
0223-5234issn
1768-3254pii
S0223-5234(19)30717-2journal_volume
181pub_type
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