Adamantam Derivatives, Part 111* : Synthesis of Some Aminoadamantanes as Novel Antitumor Agents
1
Department of Medicinal Chemistry, College Of Pharmacy, University of Mansoura, Mansoura 35516, Egypt
2
Department of Medicinal Chemistry, College Of Pharmacy, King Saud University, P.O. Box 22452, Riyadh 11495, Saudi Arabia
3
Department of Pharmaceutical Chemistry, School of Pharmacy, Universrty of Alexandria, Alexandria 21521, Egypt
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2003, 71(3), 195-209; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-19
Submission received: 8 January 2003
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Revised: 28 April 2003
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Accepted: 28 April 2003
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Published: 15 July 2003
Abstract
New series of 1-(1-adamantyl)semicarbazide 3a, 1-(1-adamantyl)4(4-subsMuted pheny1)semicarbazides 3b-e, 1-(1-adamantyl)-3-(subsMuted aminosulfonyl)ureas 5a-g, 1-(1-adamantyl)-4-(1-adamantylamino-methylene)-semicarbazide 7, 1-(1-adamantyl)-4-(1-adamantylcarbonylmethyl)semicarbazide 8, 1-(Iadamantyl)-4-acylsemicarbazides Sad and 1-(1-adamantyl)-4-(1-adamantylaminocarbonyl) thiosemicarbazide 10 have been synthesized and tested for their anMumor activity. Among them, compounds 3a, 5a, 9a. and 9d exhibited a broad spectrum antitumor activity with full panel (MG-MID) median growth inhibition (GI50) of 1 0.5, 12.0, 6.8 and 5.5 μM respectively. In addition, compounds 3a, 3c, and 5d proved to be of moderate selectivity toward leukemia cell lines wrth ratios of 3.0, 3.9 and 4.0 respectively. Moreover, compounds 5a and 5g showed moderate selectivrty toward melanoma cell lines with ratios of 3.6 and 4.4 respectively. The detailed synthesis, specroscopic and biological data are reported.
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MDPI and ACS Style
El-Sherbeny, M.A.; Youssef, K.M.; Mahran, M.A. Adamantam Derivatives, Part 111* : Synthesis of Some Aminoadamantanes as Novel Antitumor Agents. Sci. Pharm. 2003, 71, 195-209. https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-19
AMA Style
El-Sherbeny MA, Youssef KM, Mahran MA. Adamantam Derivatives, Part 111* : Synthesis of Some Aminoadamantanes as Novel Antitumor Agents. Scientia Pharmaceutica. 2003; 71(3):195-209. https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-19
Chicago/Turabian StyleEl-Sherbeny, M. A., K. M. Youssef, and M. A. Mahran. 2003. "Adamantam Derivatives, Part 111* : Synthesis of Some Aminoadamantanes as Novel Antitumor Agents" Scientia Pharmaceutica 71, no. 3: 195-209. https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-19
