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Synthesis and Bioactivity of Thiosemicarbazones Containing Adamantane Skeletons

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Drug R&D Center, Vietnam Military Medical University. No.160, Phung Hung Street., Phuc La ward, Ha Dong District, Hanoi 100000, Vietnam
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Department of Pharmaceutical Chemistry, Hanoi University of Pharmacy. No. 15, Le Thanh Tong Street, Hoan Kiem District, Hanoi 100000, Vietnam
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Hanoi University of Science and Technology. No.1, Dai Co Viet Street., Bach Khoa Ward, Hai Ba Trung District, Hanoi 100000, Vietnam
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Authors to whom correspondence should be addressed.
Molecules 2020, 25(2), 324; https://doi.org/10.3390/molecules25020324
Received: 17 December 2019 / Revised: 7 January 2020 / Accepted: 9 January 2020 / Published: 13 January 2020
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 2ac, 2f, 2g, 2j, 2k, 3g, and 3i were moderate inhibitors against MCF-7. View Full-Text
Keywords: adamantane derivatives; thiosemicarbazone; antimicrobial; cytotoxicity activity adamantane derivatives; thiosemicarbazone; antimicrobial; cytotoxicity activity
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MDPI and ACS Style

Pham, V.H.; Phan, T.P.D.; Phan, D.C.; Vu, B.D. Synthesis and Bioactivity of Thiosemicarbazones Containing Adamantane Skeletons. Molecules 2020, 25, 324.

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