Synthesis, anti‐proliferative activity, SAR, and kinase inhibition studies of thiazol‐2‐yl‐ substituted sulfonamide derivatives.

A series of novel thiazol‐2‐yl substituted‐1‐sulfonamide derivatives were synthesized from anilines. This involved the coupling of sulfonyl chlorides with thiazol amine to obtain the final compounds 7a–7j and 8a–8j. All synthesized compounds were screened for anticancer activity against MCF‐7, HeLa, A‐549, and Du‐145 cancer cell lines by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay. Preliminary bioassay suggests that most of the compounds show anti‐proliferation to different degrees, with doxorubicin used as positive control. The synthesized compounds show IC50 values in the range 2.74–8.17 μM in the different cell lines. The compounds 7d, 7e, 8a, 8d, and 8e were active compared to doxorubicin. The compounds having butyl and pantyl chains were more active than their lower and higher carbon chains and also their ring counterparts. Novel thiazol‐2‐yl substituted‐1‐sulfonamide derivatives were synthesized and identified for their anticancer activity against MCF‐7, HeLa, A‐549 and Du‐145 cancer cell lines by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay. The synthesized compound shows IC50 values in the range of 2.74‐8.17 µM in different cell lines. The compounds having butyl and pantyl chains were active compared with their lower and higher carbon chains and also with their ring counterparts. [ABSTRACT FROM AUTHOR]