Synthesis and Bioactivity of Thiosemicarbazones Containing Adamantane Skeletons.

Molecules

Drug R&D Center, Vietnam Military Medical University. No.160, Phung Hung Street., Phuc La ward, Ha Dong District, Hanoi 100000, Vietnam.

Published: January 2020

AI Article Synopsis

  • - The study involved a chemical reaction of 4-(1-adamantyl)-3-thiosemicarbazide with various substituted acetophenones and benzaldehydes, which led to the creation of thiosemicarbazones featuring adamantane structures.
  • - The resulting compounds were tested for their effectiveness against certain bacteria and fungi, showing high antifungal activity and varying degrees of antibacterial effectiveness, with some compounds performing well against Gram-positive bacteria.
  • - Notably, compounds with hydroxyl groups on the phenyl ring demonstrated strong potential as cancer-fighting agents, particularly against Hep3B, A549, and MCF-7 cancer cell lines, while others showed moderate inhibitory effects.

Article Abstract

Reaction of 4-(1-adamantyl)-3-thiosemicarbazide () 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 , and cytotoxicity against four cancer cell lines (Hep3B, HeLa, A549, and MCF-7). All of them showed good antifungal activity against . Compounds , , , and , , displayed significant inhibitory activity against . Compounds , , , and had moderate inhibitory potency against . Compounds , and found so good inhibitory effect on . Compounds and , which contain () 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 -, , , , , , and were moderate inhibitors against MCF-7.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7024387PMC
http://dx.doi.org/10.3390/molecules25020324DOI Listing

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