Objective: The series of 2-(4-Phenylamino)-N-(5-((4-nitrophenoxy)methyl) -1,3,4-oxadiazol-
2-yl)aceta-mide (5a-5e) and substituted N-(5-(Phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2-
(phenylamino)acetamide (5f-5i) was designed, synthesized and investigated for Collapsin Response
Mediator Protein 1 (CRMP 1) inhibitors as small lung cancer.
Design: Design of compounds was determined by literature review and molecular docking studies
in iGEMDOCK 2.0.
Materials and 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. The assay of telomerase in cellular extracts was modified
from the PCR-based Telomeric-Repeat Amplification Protocol (TRAP), using the oligonucleotides
TS and CX.
Results: Novel substituted 2-(4-Phenylamino)-N-(5-((4-nitrophenoxy)methyl)-1,3,4-oxadiazol-2-
yl) acetamide (5a-5e) and substituted N-(5-(Phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2-(phenylamino)
acetamide (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 5a and 5f were equipotent with respect to activity as compared to standard
Conclusion: Amongst the hybrids, p-nitro substituted derivative (5a) and p-chloro substituted (5f)
showed the highest activity against human lung cancer cell line NCI-H2066 by TRAP assay.