Synthesis Of Novel Bio-Active Molecues

Emergence of new diseases and toxic side effects/ resistance problems faced with already existing drug molecules reinvigorate to look for safer and more effective drugs. Under these circumstances it is essential to put constant efforts to make new molecules and to screen them against various diseases using various test kits.

A series of 6, 7-dialkoxy-4-anilinoquinazolines were designed, synthesized by substituting different heterocycles on 6-position and a variety of anilines on 4-position of the quinazoline. These novel quinazoline compounds were screened for their cytotoxic effect on epidermal growth factor receptor overexpressing skin epidermoid carcinoma cell line (A431), by using nonoverexpressing tumor cells as negative control (breast adeno carcinoma cell line MCF-7). 2-Butyl-4-chloro-1-{3-[7-methoxy-4-(3-(trifluoromethyl)phenylamino)quinazolin-6-yloxy]-propyl}-1H-imidazole-5-carbo- xaldehyde (1) and 2-butyl-4-chloro-1-{3-[4-(3-iodophenyl amino)-7-methoxyquinazolin-6-yloxy]propyl}-1H-imidazole-5-carboxaldehyde (2) were found to be more potent against A431 cell line (IC50 3.5 μM and 3 μM) and their activities are comparable to gefitinib. Insilico docking experiments with human EGFR Tyrosine kinase domain (PDB id-2gs2) indicated that 2 docks at the same position as that of Gefitinib involving Val702, Ala719, Ser 696, Lys721.

Synthesised prenylated flavanones and their precursors (chalcones) which are found to be anti- oxidants. All these compounds were subjected to radical scavenging and reducing power tests using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) by Blois method and by Oyaizu method respectively. Chalcones were found to have better radical scavenging as well as reducing power activity than their respective flavanones.