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Synthesis and Antitumor Activity of Novel [1,2,4,5]-tetrazepino[6,7-b] indole Derivatives: Marine Natural Product Hyrtioreticuline C and D Analogues

[ Vol. 19 , Issue. 1 ]


Zeinab A. Muhammad, Mohamed A.A. Radwan*, Thoraya A. Farghaly*, Hatem M. Gaber and Mahmuod M. Elaasser   Pages 79 - 86 ( 8 )


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 azepinoindole 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.

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


Hydrazonoyl halides, isatin, [1, 2, 4, 5]tetrazepino[6, 7-b]indoles, Hyrtioreticuline, antitumor agents, SAR study.


National Organization for Drug Control and Research (NODCAR), P.O.Box 29, Cairo, Applied Organic Chemistry Department, National Research Centre, Dokki, Giza, Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, National Organization for Drug Control and Research (NODCAR), P.O.Box 29, Cairo, The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo

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