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Synthesis, anti‐proliferative activity, SAR, and kinase inhibition studies of thiazol‐2‐yl‐ substituted sulfonamide derivatives
Author(s) -
Pawar Chandrakant D.,
Chavan Sadhana L.,
Pawar Umakant D.,
Pansare Dattatraya N.,
Deshmukh Santosh V.,
Shinde Devanand B.
Publication year - 2019
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.201800312
Subject(s) - chemistry , sulfonamide , hela , bromide , sulfonyl , doxorubicin , amine gas treating , mtt assay , cell culture , bioassay , stereochemistry , thiazole , in vitro , combinatorial chemistry , medicinal chemistry , biochemistry , organic chemistry , alkyl , medicine , surgery , chemotherapy , biology , genetics
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 IC 50 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.