Anti-HIV-1 and cytotoxicity studies of piperidyl-thienyl chalcones and their 2-pyrazoline derivatives

A series of 12 new pyrazoline derivatives was prepared from piperidyl chalcones, which in turn were synthesized by condensing 4-piperidin-1-ylbenzaldehyde with diverse acetylthiophenes. The target compounds were characterized by spectroscopic techniques (NMR, IR, MS) and elemental analysis. All the compounds were screened for cytotoxic and anti-HIV-1 activities. Compounds 1c , 1g , 1j , 2a , 2c , 2e , 2g , and 2k demonstrated potential anti-HIV activity but were cytotoxic except for 2e and 2k , which displayed no cytotoxicity in primary human cells. Bioassay results show that the type and positions of the substituents seem to be critical for their cytotoxic and anti-HIV-1 activities.