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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis, Cytotoxic and Phytotoxic Effects of Some New N4-Aryl Substituted Isatin-3-thiosemicarbazones

Author(s): Humayun Pervez, Muhammad Ramzan, Muhammad Yaqub and Khalid Mohammed Khan

Volume 8, Issue 5, 2011

Page: [452 - 458] Pages: 7

DOI: 10.2174/157018011795514159

Price: $65


A series of N4-aryl substituted isatin-3-thiosemicarbazones was prepared by the reaction of isatin with an appropriate thiosemicarbazide in ethanol containing a few drops of acetic acid. The newly synthesized compounds were characterized by means of their analytical (CHN) and spectral (IR, 1H-NMR, EIMS) data, and evaluated for their cytotoxicity and phytotoxicity potential. Eleven out of thirteen compounds tested proved to be active in the brine-shrimp lethality bioassay exhibiting significant cytotoxic activity with LD50 values ranging from 1.75x10-5M to 1.91x10-4M. In phytotoxicity assay, all the synthesized compounds, regardless of the nature of aryl substituents, demonstrated weak to moderate (5-30%) plant growth inhibition at the highest tested concentration (500 μg/mL).

Keywords: Isatin, Isatin Derivatives, Thiosemicarbazones, Isatin-3-thiosemicarbazones, Cytotoxicity, Phytotoxicity, Cytotoxic, Phytotoxic, N4-Aryl, CHN, antiplasmodial, antitubercular, anticonvulsant, anxiogenic, anthelmintic

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