Synthesis,anti‐proliferative activity,SAR, and kinase inhibition studies of thiazol‐2‐yl‐ substituted sulfonamide derivatives |
| |
Authors: | Chandrakant D Pawar Sadhana L Chavan Umakant D Pawar Dattatraya N Pansare Santosh V Deshmukh Devanand B Shinde |
| |
Abstract: | 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. |
| |
Keywords: | anticancer cyclization kinase inhibitors sulfonamide thiazol‐2‐yl |
|
|