Synthesis and antitumor activity of novel [1,2,4,5]-tetrazepino[6,7-b]indole derivatives: Marine natural productHyrtioreticuline C and D analogues.

BACKGROUND: Several biologically active indole alkaloids have been isolated from marine organisms over the previous few years. Many scientsts interested in synthesis of the marine azepino-indole alkaloids due to their wide range of bioliogical activies.

OBJECTIVE: We interested herein to synthesize a new series of some analogues of new naturally occurring azepinoindole alkaloids.

METHOD: A novel series of [1,2,4,5]tetrazepino[6,7-b]indoles, Marine natural product Hyrtioreticuline C and D analogues, were synthesized via the reaction of 3-hydrazonoindolin-2-one with hydrzaonoyl chlorides in basic medium.

RESULTS: The spectral data of the products proved their structure. All new derivatives were tested against two carcinoma cell lines ((A-549 & HepG2)) in comparison with the well-known anticancer standard drug (cisplatin) and two derivatives from the tested compounds showed activity more potent than the reference drug.

CONCLUSIONS: We succeeded in synthesis of new antitumor active azepinoindole alkaloids.