- Synthesis and biological activities of nicotinaldehyde based azlactones
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A series of nicotinaldehyde based azlactones 3a-g, 6a-f, 11a-d, 16b-c, and 16e-f have been prepared and screened for their free radicals scavenging, a-glucosidase inhibitory and anti-proliferative activities on cell lines, namely lung adenocarcinoma (A549), human breast cancer (MCF7) and human epithelial cervical cancer (HeLa). Compound 3g is the most potent α-glucosidase inhibitor followed by compounds 6b and 6a. Compound 11b is the better DPPH and ABTS+radical scavenger. Compounds 11c-d and 16f show anti-proliferative activity on all the tested cell lines. However, compounds 16c and 16e display anti-proliferative activity on MCF7 and HeLa cell lines.
- Dayakar,Mounika,Rajkumar,Zehra,Murthy,Kalivendi, Shasi V.,Tiwari,China Raju
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- Synthesis and quantitative structure-activity relationships study for phenylpropenamide derivatives as inhibitors of hepatitis B virus replication
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A series of new phenylpropenamide derivatives containing different substituents was synthesized, characterized and evaluated for their anti-hepatitis B virus (HBV) activities. The quantitative structure eactivity relationships (QSAR) of phenylpropenamide compound have been studied. The 2D-QSAR models, based on DFT and multiple linear regression analysis methods, revealed that higher values of total energy (TE) and lower entropy (Sθ) enhanced the anti-HBV activities of the phenylpropenamide molecules. Predictive 3D-QSAR models were established using SYBYL multifit molecular alignment rule. The optimum models were all statistically significant with cross-validated and conventional coefficients, indicating that they were reliable enough for activity prediction.
- Yang, Jing,Ma, Min,Wang, Xue-Ding,Jiang, Xing-Jun,Zhang, Yuan-Yuan,Yang, Wei-Qing,Li, Zi-Cheng,Wang, Xi-Hong,Yang, Bin,Ma, Meng-Lin
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