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Reaction of 4-(1-adamantyl)-3-thiosemicarbazide ( 1 ) with numerous substituted acetophenones and benzaldehydes yielded the corresponding thiosemicarbazones containing adamantane skeletons. The synthesized compounds were evaluated for their in vitro activities against some Gram-positive and Gram-negative bacteria, and the fungus Candida albicans , and cytotoxicity against four cancer cell lines (Hep3B, HeLa, A549, and MCF-7). All of them showed good antifungal activity against Candida albicans . Compounds 2c , 2d , 2g , 2j and 3a , 3e , 3g displayed significant inhibitory activity against Enterococcus faecalis . Compounds 2a , 2e , 2h , 2k and 3j had moderate inhibitory potency against Staphylococcus aureus . Compounds 2a , 2e and 2g found so good inhibitory effect on Bacillus cereus . Compounds 2d and 2h , which contain ( ortho ) hydroxyl groups on the phenyl ring, were shown to be good candidates as potential agents for killing the tested cancer cell lines, i.e., Hep3B, A549, and MCF-7. Compounds 2a - c , 2f , 2g , 2j , 2k , 3g , and 3i were moderate inhibitors against MCF-7.

A series of simple (6-substituted benzothiazol-2-yl)acrylamides was synthesized and evaluated for cytotoxicity and antimicrobial effects. All six compounds displayed very significant cytotoxicity against four cancer cell lines tested including A549 (a human lung cancer cell line), Hela (a human ovarian cancer cell line), MCF7 (a human breast cancer cell line), and even MCF7-ADR (adriamycin-resistant human breast cancer cell line), with IC(50) values in microgram/ml range and as low as 0.66 μg/ml. The synthesized compounds also exhibited some antifungal effects against Apergillus niger.