Synthesis, Method Optimization, In-Vitro Antitumor Activity Of Some New Substituted Quinazoline And Quinazolin-4-One Derivatives: Search For Anticancer Agent

Abstract

The essence of work is to synthesize some New 2,4 disubstituted Quinazoline and 2,3 disubstituted Quinazolin-4-one derivatives and to test them for their In-vitro anticancer activity. Two different starting materials namely Anthranilamide and Anthranilic acid were used to obtain two different intermediate one Benzamide intermediate and the second one Benzoxazine-4-one as an intermediate which lead to two different novel Quinazoline and Quinazolin-4-one derivatives and its further substitution gave a series of novel compounds. In the light of above, 2^nd and 4^thposition of quinazoline ring nucleus and 2^nd and 3^rdposition of quinazolin-4-one were explored to obtain different derivatives. Novel 4-Anilino Quinazoline derivatives and Schiff bases were prepared from reaction scheme 1 and various 2-substituted amino thiadiazole quinazoline-4-one derivatives were synthesized from reaction scheme 2.We have applied the methodology of fusion for the synthesis of 2-substituted amino thidadiazole-2-(4-nitrophenyl) quinazoline 4(3H)-one 6(a-d) at 250-260 ⁰C, instead of using organic solvent, to by pass the problem of ring opening, which is usually observed while synthesizing quinazolines  from bentranil or benzooxazin-4-one. Fusion method is easy, more expedient, eco-friendly process and time saving method. It is a pace towards green chemistry.

To summarize, we have prepared 06 new 2,4 disubstituted quinazoline derivatives from reaction scheme 1 and 04 new 2,3 disubstituted Quinazolin-4-one derivatives from reaction scheme 2 successfully and evaluated them for their anticancer activity.