| Summary: | A one-pot, single-step, and an atom-economical process towards the synthesis of highly functionalized spirooxindoles analogues was efficiently conducted to produce a satisfactory chemical yields (70−93%) with excellent relative diastereo-, and regio-selectivity. An in vitro antiproliferative assay was carried out on different cancer cell lines to evaluate the biological activity of the synthesized tetrahydro-1’<i>H</i>-spiro[indoline-3,5’-pyrrolo[1,2-<i>c</i>]thiazol]-2-one <b>5a−n.</b> The prepared hybrids were then tested <i>in vitro</i> for their antiproliferative effects against three cancer cell lines, namely, HepG2 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer). The spirooxindole analogue <b>5g</b> exhibited a broad activity against HepG2, MCF-7, and HCT-116 cell lines of liver, breast, and colorectal cancers when compared to <i>cis</i>platin. Modeling studies including shape similarity, lipophilicity scores, and physicochemical parameters were calculated. The results of this study indicated that spirooxindole analogue <b>5g</b> retained a good physiochemical parameters with acceptable lipophilicity scores.
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