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
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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 (GI
50) 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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