Molecules 2012, 17(8), 9868-9886; doi:10.3390/molecules17089868
Article

Synthesis and Bioactivity Evaluation of New 6-Aryl-5-cyano Thiouracils as Potential Antimicrobial and Anticancer Agents

Azza Taher Taher 1 email and Sahar Mahmoud Abou-Seri 2,* email
1 Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, P.O. Box, 11562, Egypt 2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, P.O. Box, 11562, Egypt
* Author to whom correspondence should be addressed.
Received: 16 July 2012; in revised form: 25 July 2012 / Accepted: 10 August 2012 / Published: 17 August 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract: Several novel 6-aryl-5-cyano thiouracil derivatives were synthesized and explored for their activities as antibacterial, antifungal and anticancer agents. The antimicrobial evaluation revealed that compounds 7b and 7c possessed superior antibacterial activity against the Gram positive bacteria S. aureus and B. subtilis compared to the reference drug amoxicillin. Moreover, compound 4i was found to be a broad spectrum antimicrobial agent and it also exhibited the highest antifungal activity against C. albicans, even higher than the reference drug amphotericin B (MIC = 2.34, 3.00 μg/mL respectively). Selected compounds were tested for in vitro cytotoxicity at a single 10−5 M concentration in accordance to the NCI (USA) protocol. The preliminary screening results showed that most of the compounds had limited cytotoxic activity against renal cancer UO-31 and/or A498 cell lines. Nevertheless, compounds 6d and 6i displayed potent growth inhibitory effect toward non-small cell lung cancer HOP-92 and leukemia MOLT-4 cell lines, respectively.
Keywords: 6-aryl-5-cyano thiouracils; antibacterial; antifungal; anticancer

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MDPI and ACS Style

Taher, A.T.; Abou-Seri, S.M. Synthesis and Bioactivity Evaluation of New 6-Aryl-5-cyano Thiouracils as Potential Antimicrobial and Anticancer Agents. Molecules 2012, 17, 9868-9886.

AMA Style

Taher AT, Abou-Seri SM. Synthesis and Bioactivity Evaluation of New 6-Aryl-5-cyano Thiouracils as Potential Antimicrobial and Anticancer Agents. Molecules. 2012; 17(8):9868-9886.

Chicago/Turabian Style

Taher, Azza Taher; Abou-Seri, Sahar Mahmoud. 2012. "Synthesis and Bioactivity Evaluation of New 6-Aryl-5-cyano Thiouracils as Potential Antimicrobial and Anticancer Agents." Molecules 17, no. 8: 9868-9886.

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