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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