ULTRASOUND-ASSISTED SYNTHESIS AND DOCKING STUDY OF NOVEL CHROMONE-THIADIAZOLE INTEGRATED PHOSPHONATE DERIVATIVES TARGETING TOPOISOMERASE II AS ANTICANCER AGENTS

Objective: The present studies discuss the anticancer activity of different topoisomerase II inhibitors with docking study.
 Methods: work reports synthesis novel diethyl (4-oxo-4H-chromen-3-yl)(5-substituted phenyl-1,3,4-thiadiazol-2-ylamino)methyl phosphonate derivatives 6(a-j). They were synthesized through one-pot three-component Kabachnik-Fields reaction by using ultrasonicator processor, at room temperature in presence Zirconium oxychloride (ZrOCl2).
 Results: structures compounds confirmed spectral analysis. 6(a-j) evaluated for their vitro against human cancer cell lines such as DU 145 (Human Prostate Cancer) and MCF-7 (Breast cancer) also on non-tumor MCF-10 (normal breast epithelial cell) MTT assay. From screening results data, compound 6e was found to be most potent among IC50 value 2.97 µM 3.11 µM, respectively. 6h has shown cycle arrest G2/M phase, along decrease cells G0/G1 phage. able induce apoptosis lines. further inhibitory activity.
 Conclusion: result assay, study shows that synthesised derivative are active agent MCF-10, DU-145 line.