Design, Synthesis, and In Vitro Antileishmanial and Antitumor Activities of New Tetrahydroquinolines

Madkour H. ; El-Hashash M. ; M. S. Salem ; Mahmoud A. ; Al kahraman Y. 


Abstract


© 2017 Wiley Periodicals, Inc. A novel series of tetrahydroquinolines containing acetohydrazide, oxopyrazole, oxothioxodihydropyrazole, and thioxotriazole have been synthesized. Antileishmanial, antitumor, and cytotoxicity activities of synthesized compounds were evaluated in vitro. Antileishmanial activity of the most synthesized compounds showed tremendous activity towards Leishmania major. Most of the test compounds exhibited significant level of tumor inhibition. The tetrahydropyrano[2,3-b]quinolin-2-one 6 and 4-oxo-4H-pyrazol-3-yloxytetrahydroquinoline-3-carbonitrile derivatives 18 showed 100% tumor inhibition comparable with standard drug vincristine (100% tumor inhibition). Tetrahydroquinolines under investigation showed cytotoxicity with LD50values in the range 0.56–3.01 μg/mL compared with standard drug MS-222 with LD50value of 4.30 μg/mL. The presence of a pyrazole ring markedly improved the activity profiles of tetrahydroquinoline. All newly synthesized compounds were characterized by IR,1H NMR, and MS.


Other data

Issue Date 1-Feb-2018
Journal Journal of Heterocyclic Chemistry 
URI http://research.asu.edu.eg/handle/123456789/167675
DOI 2
https://api.elsevier.com/content/abstract/scopus_id/85038241721
391
55
10.1002/jhet.3046


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