New alpha-(N)-heterocyclichydrazones: evaluation of anticancer, anti-HIV and antimicrobial activity.
A series of 3- and 5-methylthiophene-2-carboxaldehyde alpha-(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 microM. 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
Luisa
L
Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, Università degli Studi di Siena, 53100 Siena, Italy. savini@unisi.it
Chiasserini
Luisa
L
Travagli
Valter
V
Pellerano
Cesare
C
Novellino
Ettore
E
Cosentino
Sofia
S
Pisano
M Barbara
MB
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004354:Drug Screening Assays, Antitumor; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure
D000900:Anti-Bacterial Agents; D019380:Anti-HIV Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D006835:Hydrazones