A series of 3- and 5-methylthiophene-2-carboxaldehyde a-(N)-heterocyclichydrazones were synthesized and submitted to an in vitro investigation of their anticancer, anti-HIV and antimicrobial activities. Some of the newly synthesized compounds were found to possess antiproliferative properties, whereas no anti-HIV activity was seen; the most active of the series was the derivative 2i, which exhibited tumour growth inhibition activity against all cell lines displaying GI50 values between 1.63 and 26.5 µM. The title compounds were generally ineffective against Gram-positive and Gram-negative bacteria, while showed a moderate antifungal activity against C. albicans and A. fumigatus.
Savini, L., Chiasserini, L., Travagli, V., Pellerano, C., Novellino, E., Cosentino, S., et al. (2004). New alpha-(N)-heterocyclichydrazones: evaluation of anticancer, anti-HIV and antimicrobial activity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 39(2), 113-122 [10.1016/j.ejmech.2003.09.012].
New alpha-(N)-heterocyclichydrazones: evaluation of anticancer, anti-HIV and antimicrobial activity
Savini, Luisa;Chiasserini, Luisa;Travagli, Valter;Pellerano, Cesare;
2004-01-01
Abstract
A series of 3- and 5-methylthiophene-2-carboxaldehyde a-(N)-heterocyclichydrazones were synthesized and submitted to an in vitro investigation of their anticancer, anti-HIV and antimicrobial activities. Some of the newly synthesized compounds were found to possess antiproliferative properties, whereas no anti-HIV activity was seen; the most active of the series was the derivative 2i, which exhibited tumour growth inhibition activity against all cell lines displaying GI50 values between 1.63 and 26.5 µM. The title compounds were generally ineffective against Gram-positive and Gram-negative bacteria, while showed a moderate antifungal activity against C. albicans and A. fumigatus.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
https://hdl.handle.net/11365/25759
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