Baylis-Hillman adduct-derived <i>N</i>-cinnamyl-substituted isatin derivatives were synthesized and evaluated for their antitubercular activity on <i>Mycobacterium tuberculosis</i> H<sub>37</sub>Rv strain ATCC 27294 by agar dilution method. Anticancer activity for the same compounds was also screened on four different cell lines: Chinese hamster ovary (CHO cells), Colo 205 (human colon cancer), Sup-T1 (human lymphoma) and C6 glioma (rat glioma) by MTT assay method. The compounds (<b>3j</b>-<b>l</b>) have shown significant activity against <i>Mycobacterium</i> strain and the compound <b>3l</b> has shown specific cytotoxic activity.