Ishan Pachal
Parul University, India
Title: Synthesis and Biological Evaluation of New 1,3,4-Oxadiazole derivatives as anticancer agent
Biography
Biography: Ishan Pachal
Abstract
Objective: The present work deals with the design, synthesis, characterization of novel substituted 2-(4-phenylamino)-N-(5-((4-nitrophenoxy)methyl)-1,3,4-oxadiazol-2-yl)acetamide (RRC 5a-5e) and substituted N-(5-(phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2-(phenylamino)acetamide(RRC 5f-5i) derivatives as small lung cancer.
Methods: Novel 1, 3, 4 Oxadiazole derivatives were synthesized and characterized by melting point, TLC, IR Spectroscopy, Mass spectroscopy and 1H NMR. In vitro biological evaluation was performed on NCI-H2066 cell line for different concentrations 10-1000µM by telomeric repeat amplification protocol assay.
Results: Novel substituted 2-(4-phenylamino)-N-(5-((4-nitrophenoxy)methyl)-1,3,4-oxadiazol-2-yl)acetamide (RRC 5a-5e) and substituted N-(5-(phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2-(phenylamino)acetamide(RRC 5f-5i) were synthesized, and characterized using spectral and analytical data. All compounds have shown considerable % inhibition of Cell Growth with respect to Bevacizumab, but compound RRC 5a and RRC 5f are equipotent with respect to activity as compared to standard Bevacizumab. IC50 value of RRC 5a and RRC 5f are 33.05μM and 35.58μM concentration respectively.
Conclusion: Among the hybrids, p-Nitro substituted derivative (RRC 5a) and p-Chloro substituted (RRC 5f) showed highest activity against human lung cancer cell line NCI-H2066 by TRAP assay.
Key Words: Oxadiazole, NCI-H2066, cell line, TRAP assay