International Journal of Pharmaceutical Investigation, 2020, 10, 4, 594-603.
Published: December 2020
Type: Original Article
College of Pharmaceutical Sciences, School of Health Sciences, Dayananda Sagar University, Bangalore, Karnataka, INDIA.
Faculty of Pharmaceutical Sciences, PES University, Bangalore, Karnataka, INDIA.
Objectives: Heterocyclic compounds are enormously widespread in nature and have attracted research interest because of their pharmaceutical and biological properties. Amongst the heterocyclic rings, the thiazoles are the most important building blocks in today’s drug discovery and are found to have extensive biological activities against different types of diseases. Many potent anti-cancerous drugs like Tiazofurin are having 1,3 thiazole as an active ring structure and based on this theory, a new series of 2, 4 di substituted 1,3 thiazole derivatives were synthesized. Methods: First 2-amino-4-substituted phenyl thiazoles were synthesized by adapting a well-known Hantzsch reaction and subsequently 2-amino substituted derivatives were synthesized using various aryl aldehydes by following established Schiff’s reaction. The synthesized compounds were confirmed by TLC, IR, HNMR, CNMR and Mass Spectral Analysis. Then all the synthesized compounds were docked to RAS p21 receptor using PATCH DOCK Software to study their anti-cancerous activity. Then the compounds were screened for cancer cell line studies. Results: All the synthesized compounds exhibited some degree of anti-cancerous activity both in docking studies and in vitro anti-cancerous cell line studies. Conclusion: Amongst all the 16 synthesized, most compounds showed moderate to good anti-cancerous activity and the compounds S3P1c, S3P2c, S3P2d, S3P3a and S3P4d have shown the best activity.
Keywords: Thiazole, Hantzsch, Docking, Cancer cell line.