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A series of novel acridine-thiazole bridged coumarin derivatives  3a–3i  were designed, synthesized and subjected for their  in-vitro  antiproliferative activity on human breast cancer (MDA-MB-231), lung cancer (A-549) and colon cancer (HT29) cell lines. In case of human breast (MDA-MB-231) cell line, among the nine screened compounds,  3d ,  3c ,  3g , and  3a  exhibited moderate to good antiproliferative activity with IC 50  values in the range 14.06–8.03 µM concentration. The compound  3d  exhibited higher activity with IC 50  value 8.03 µg/mL, compared to  3c  with IC 50  value of 12.03 µg/mL. Whereas, compounds  3g ,  3b ,  3h ,  3a , and  3i  also exhibited significant cytotoxicity with IC 50  values in the range 05.18–18.17 µM concentration. Further, the compound  3g  exhibited distinct activity with IC 50  value 05.18 µg/mL, followed by compound  3b  with IC 50 value of 09.09 µg/mL for A-549 cancer cell line. However, for HT29 cell line all of the compounds showed significantly lesser activity when compared with standard drug Cisplatin. In addition, the synthesized compounds were screened for their anti-TB activity and its cytotoxicity, the compound  3g  exhibited excellent antitubercular activity with MIC of 0.78 µg/mL, while the compound  3b  exhibiting MIC of 1.56 µg/mL with the highest safety percentage survival of 72% and 78%.

Design and Synthesis of Polycyclic Acridin-(9-yl-Amino)Thiazol-5-yl)-2H-Chromen-2-One Derivatives: As Antiproliferative and Anti-TB Pharmacophores