Cancer tends to be one of the major diseases in the present century affecting global population, and proliferation of cancerous cells needs to be eliminated as the cell growth is uncontrolled. In this present study, a series of facile, high yielding 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-ones 3(a-j) was designed, synthesized and evaluated for anti-proliferative activity against different human cancer cell lines; MCF-7 (breast cancer), K562 (leukemic cancer), HeLa (cervical cancer), Colo205 (colorectal adreno carcinoma), HepG2 (Hepato cellular carcinoma) cell lines. The compounds 3a, 3c, 3d, 3e, 3f, 3g and 3j exhibited an average inhibition of 35% against Hepatocellular Carcinoma (Hepg2) cell lines whereas, compounds 3a, 3c, 3d and 3e exhibited 33, 31, 35 and 33% inhibition, respectively, against HeLa cells at 10 μm concentrations. Doxorubicin was employed as a positive control. The ADME-TOX data was obtained by subjecting the molecules in silico to quantitatively predict the physicochemical properties. The structure of the title compounds were established by IR, 1 H NMR, 13 C NMR and Mass analysis.
Pancreatic cancer is the most severe, as a consequence of asymptomatic nature and ineffective therapies among all malignancies. Nicotinamides are effective ring systems in the treatment of pancreatic cancer with their wide range of applications. In the present investigation, nicotinamide and 4‐cyanophenyl ring systems are brought together to obtain greater potency. For the process of investigation, PARP1 protein is targeted and evaluated by docking at the active site to determine the protein‐ligand interaction, revealed the potential with the binding affinity of −9.0 to −11.0 Kcal/mol to inhibit the poly ADP‐ribose polymerase 1 (PARP1) pathway. The MTT‐assay assessment of a synthesized series has been performed against Capan‐1 pancreatic cancer cell line. The nicotinamide compounds demonstrated a significant inhibitory effect over Capan‐1 cell line, and 6‐(4‐cyanophenyl)‐N‐(3‐phenylpropyl)nicotinamide exhibited as a potential lead for the development of novel chemotherapeutics against pancreatic cancer.
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