Abstract

AbstractA series of new pyrazolothiazole hybrids were designed and synthesized by the microwave‐assisted multicomponent reaction of thiosemicarbazide, 3‐(furan‐2‐yl)‐1‐(pyridin‐2‐yl)prop‐2‐en‐1‐one and 1‐(pyridin‐2‐yl)‐3‐(thiophen‐2‐yl)prop‐2‐en‐1‐one with substituted 2‐bromoacetophenones. Structures of all the synthesized compounds were in good agreement with their spectral (FTIR, 1H & 13C NMR, Mass) and analytical data (CHN analysis). The target compounds were screened for their in vitro cytotoxic activity by testing against human adenocarcinoma (A549), cervical cancer (HeLa), human neuroblastoma (SK−N‐SH) and human prostate cancer (DU‐145) cell lines. From the in vitro results, it was found that the compound derived from p‐ NO2 phenyl (4 h) has potent activity against HeLa cell line with IC50 value 9.97 ± 0.05 μM. Also, the compounds having p‐OCH3 phenyl (4 c), phenyl (4 i), and p‐Cl phenyl (4 j) substitutions exhibited significant activity against HeLa cell line with IC50 values 19.78 ± 0.03 μM, 18.47 ± 0.01 μM and 15.61 ± 0.06 μM respectively.

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