Objective: Novel anticancer agents were designed to be synthesized comprising the essential features for anticancer activity considering Leucettamine B as a lead compound. Method: 3-Phenyl-2-thioxoimidazolidin-4-one 1 has been utilized for synthesis of various fused pyrrolo[1,2-e]imidazole 4, 8a,b, 11, 14, 16, 18, 20, 21, 23, 25 analogues through different chemical reactions. Results: Structures of these compounds were confirmed by spectral and elemental analyses Thirteen of the newly synthesized compounds were selected by the NCI – Maryland-U.S.A. and were tested for their anticancer activity in an initial single high dose in the full NCI 60 cell line panel. Conclusion: 5-amino-2,3,7,7a-tetrahydro-7-(4-methoxyphenyl)-1-oxo-2-phenyl-3-thioxo-1H-pyrrolo[1,2-e]imidazole-6-carbonitrile; 4, 1-(7-(4-chlorophenyl)-3,7-dihydro-1,5-dihydroxy-2-phenyl-3-thioxo-2H-pyrrolo[1,2-e]imidazol-6yl) ethenone; 21, were found to possess very selective potent anticancer activity against certain cancer cell lines.