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Design, Synthesis, and Anticancer Activity of Novel Benzothiazole Analogues
Author(s) -
Hassan Aisha Y.,
Sarg Marwa T.,
Hussein Ebtehal M.
Publication year - 2019
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3524
Subject(s) - benzothiazole , chemistry , cancer cell lines , in vitro , stereochemistry , cell culture , combinatorial chemistry , lead compound , structure–activity relationship , cancer , cancer cell , biochemistry , medicine , biology , genetics
On the pharmaceutical account of the reported anticancer activity of benzothiazole derivatives, differently substituted benzothiazole derivatives 2a – c to 34a , b , attached at 2‐position to different heterocyclic moieties, were synthesized via different chemical reactions. Thirteen of the newly synthesized compounds were selected by the National Cancer Institute, Bethesda, Maryland, USA, and evaluated for their in vitro antitumor activity against 60 human tumor cell lines in a one‐dose screening panel among which two compounds 4 and 17 showed high activity and were selected for further evaluation in the five‐dose full panel assay, in which compound 4 exerted powerful growth inhibitory activity against all cell lines with GI 50 ranging from 0.683 to 4.66 μM/L in addition to excellent lethal activity against most of the cell lines.