Synthesis and biological evaluation of amide derivatives of the quinazoline tethered (pyridyl)-1,2,4-thiadiazoles as anticancer agents

Abstract

A new library of amide derivatives of quinazoline-1, 2, 4-thiadiazoles (12a–j) has been synthesized and its structures were confirmed by ¹H NMR, ¹³C NMR and mass spectral data. The in-vitro anticancer activity of all the newly derived compounds (12a–j) was assessed for their preliminary anticancer applications toward different cancer cell lines including MCF-7 (breast cancer), A549 (lung cancer), Colo-205 (colon cancer) and A2780 (ovarian cancer) by employing the MTT method using Etoposide as a positive control. From the table the results indicated that most of the tested compounds displayed good to moderate activity compared to etoposide. Among the twelve compounds synthesized, compounds 12a, 12b, 12c, 12d, 12e and 12f possessed more potent activity than the positive control. Particularly, compound 12a displayed superior anticancer activity.

Graphical Abstract

Keywords:

• Amide and anticancer activity
• lapatinib
• ponatinib
• quinazoline

Acknowledgments

The authors are thankful to School of Applied Sciences, REVA University, Bangalore, Karnataka for constant encouragement during this research program for providing basic research facility.

Disclosure statement

No potential conflict of interest was reported by the author(s).