Aromatase Inhibitory Profile of Novel Tetrabromoisoindoline Derivatives

Tetrabromophthalic anhydride reacts with p-amino benzoates namely p-amino methyl benzoate and p-amino ethyl benzoate to afford isoindoline derivatives 1a,b. Also, isoindoline derivative 1a reacts with hydrazine hydrate to form benzohydrazide derivative 2. Compound 2 reacts with different aromatic aldehydes namely p-chloro benzaldehyde, p-floro benzaldehyde, and p-N,N-dimethylamino benzaldehyde to afford isoindoline derivatives 3a-c. Benzohydrazide derivative 2 reacts with ribose, and glucose to form isoindoline derivatives 4a,b. Compounds 4a,b is acetylated with acetic anhydride to give acetylated sugar derivatives 5a,b. Benzohydrazide derivative 2 reacts with potassium thiocyanate to afford triazole derivative 6. Isoindoline derivative 6 reacts with chloroacetyl chloride to afford thiazole derivative 7 which reacts with p-chlorobenzaldehyde to form isoindoline derivative 8. Isoindoline derivative 2 reacts with carbon disulfide to afford carbodithioate 9 which interacts with hydrazine hydrate to afford triazole derivative 10. Trizole derivative 10 reacts with p-chlorobenzaldehyde to afford isoindoline derivative 11. Benzohydrazide derivative 2 reacts with iosthiocyanate derivatives namely benzylisothiocyanate and phenyl isothiocyanate to give triazole derivative 12a,b. Aromatase inhibitory effect, and cytotoxic effect against T47D, and MRC-5 of isoindoline derivatives 1a,b-12a,b were reported.