Synthesis of 4-phenyl-5, 6-dihydrobenzo[h]quinazolines and their evaluation as growth inhibitors of carcinoma cells. Issue 22 (15th February 2016)

• Record Type: Journal Article
• Authors: Maurya, Hardesh K.; Hasanain, Mohammad; Singh, Sarita; Sarkar, Jayanta; Dubey, Vijaya; Shukla, Aparna; Luqman, Suaib; Khan, Feroz; Gupta, Atul
• Is Part Of: RSC advances. Volume 6:Issue 22(2016)
• Page Start: 18607
• Page End: 18618
• Publication Date: 2016-02-15
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c5ra24429c
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : The synthesis of various benzo[ h ]quinazoline analogs was accomplished through the reaction of chalcone with guanidine. The synthesized compounds were screened for their anticancer potential against different cancer cells. Abstract : The synthesis of various benzo[ h ]quinazoline analogs (4a–f, 6a–d, 8a and8b ) was accomplished through the reaction of chalcone with guanidine. The synthesized compounds (4a–f, 6a–d, 8a and8b ) were screened for their anticancer potential against different cancer cells viz MCF-7, DLD1, A549, DU145 & FaDu cell lines. Compounds4a, 6a–d &8b showed significant anticancer activity in these cancer cell lines with a range of IC50 values of 1.5–12.99 μM. A functional study of promising molecule6d at 7 μM (at the IC50 value) over 24 and 48 h showed that it possesses anticancer activity through triggering apoptosis. In a tubulin polymerization assay, 6d effectively inhibited tubulin polymerization with an IC50 of 2.27 μM. In silico docking studies of6d revealed that6d has good affinity with an estrogen receptor as well as a tubulin protein on its β-sheet of the colchicines binding site.