Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents

Chalcone: A Privileged Structure in Medicinal Chemistry

“…For example, chalcone–amidobenzothiazole conjugates ( 107 and 108 ) have been shown to exhibit potent activities against different cancer cell lines in the range 0.85–3.3 μM and induced cell cycle arrest at the G2/M phase. 351 A chalcone–platinum(II) complex ( 109 ) has been found to exhibit an excellent antitumor effect against a panel of 21 cancer cell lines, similar to the activity of its parent chalcone but different in long-term treatment and slightly different in the mechanism of apoptosis induction. 352 This hybrid containing a cisplatin moiety shows promising activity, although no in vivo data has been published.…”

“…These compounds were originally predicted to bind to tubulin at the colchicine-binding site, which has been confirmed via in vitro competition binding assays. 298,351,380–384 Very recently, a series of novel indole– chalcone derivatives were synthesized and evaluated for their antiproliferative activity. 76 Among these indole–chalcones, compound 133 has exhibited IC 50 values of 3–9 nM against six cancer cell lines, similar activities against resistant cancer cells, and low toxicity toward normal human cells.…”

A comprehensive review in current developments of benzothiazole-based molecules in medicinal chemistry

“…Compounds (72,73) polymerization and immuofluorescence analysis showed that these compounds effectively inhibit microtubule assembly at both, molecular and cellular levels, in A549 cells [115]. 2-Phenyl BTA linked imidazole moiety were prepared and evaluated for anticancer activity against different human cancer cells.…”

Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability

“…29,30 In particular, the targeting of tubulin polymerization by new diversified ligands based on CA4 and E7010 have led to promising and interesting results. 31 Herein, we describe different modifications on CA4 scaffold, specifically the incorporation of benzimidazole and benzothiazole moieties of pharmacological relevance by replacement of ring B.…”