Online ISSN: 2515-8260

Author : Ashok Baghel, Mangilal Chaudhary, Pawan Tiwari, Vinod Patidar, Dharmendra Shrivastav,


Design, synthesis and Docking Based Studies of Combretastatin analog as anti-cancer activity

Pawan Tiwari, Vinod Patidar, Dharmendra Shrivastav, Ashok Baghel, Mangilal Chaudhary

European Journal of Molecular & Clinical Medicine, 2020, Volume 7, Issue 1, Pages 4638-4649

series of substituted 6-bromo-3-(3-chloro-2-oxo-4-arylazetidin-1-yl)-2-methylquinazolin-4(3H)-onehas been synthesized and evaluated for their biological activity. The title compounds (G1-G10) were prepared by the reaction of 5-bromo anthranilic acid with acetic anhydride to form 6-bromo-2-methyl-4H-benzo[1,3]oxazin-4-one which upon treatment with hydrazine hydrate in the presence of anhydrous pyridine form 3-amino-6-bromo-2-methylquinazolin-4(3H)-one. This resulting intermediate undergoes Schiff reaction with different aromatic aldehyde followed by reflux with chloroacetylchlorideand triethylamine. Ten different quinazoline derivatives (G1-G10) were synthesized. Structural assignments of these compounds have been made by elemental analysis, FTIR, 1HNMR and Mass spectral data and the purity of the compounds was determined by TLC. All synthesized compounds have been tested for their anti-inflammatory activity by using diclofenac sodium as a standard drug. Most of the compounds showed a moderate degree of potent anti-inflammatory activity. The study concluded that the compound G3& G8were found to exhibit significant anti-inflammatory activity when compared to standard drug.