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Wanda Nawrocka 1Hanna Liszkiewicz 1Andrzej Dryś 2Joanna Wietrzyk 3Adam Opolski 3

1. Akademia Medyczna, Katedra Technologii Leków, Nankiera 1, Wrocław 50-140, Poland
2. Akademia Medyczna, Katedra Chemii Fizycznej, Nankiera 1, Wrocław, Wrocław 50-140, Poland
3. IITD PAN, Wrocław, Weigla 12, Wrocław 53-114, Poland


New esters 8-10 and hydrazones 4-6 were synthesized from 1-phenyl-2-(4-aryl-1,3,4,5-tetrahydropyrido[2,3-b][1,4]diazepin-2-ylidene)ethanones (1-3). Subsequent treatment of hydrazone 4 with p-chlorobenzaldehyde furnished azine 7. The prolonged heating of ester 8 with hydrazine hydrate afforded a polyheterocyclic compound with fused and bridged rings 12. The structures of new compounds were determined by analytical and spectral (IR, 1H NMR, MS) methods. Compounds 8 - 10 and 12 were examined for their antiproliferative activity in vitro against the cells of 5 human cancer cell lines, using SRB or MTT technique. One out of all tested compounds 12 revealed cytotoxic activity in vitro against all cell lines applied with ID50 (inhibitory dose 50%) values lower than 4 mg/ml, which is an international activity criterion for synthetic compounds. All compounds inhibits the proliferation of HL-60 human promyelocytic leukemia cell line . Carbamates 9 and 10 were active only against two cancer cell lines, namely HL-60 leukemia and HCV-29T urinary bladder cancer. Compound 8 revealed activity only against HL-60 leukemia cells.



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Related papers

Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Wanda Nawrocka
See On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2006-04-11 07:53
Revised:   2009-06-07 00:44