Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents

Synthesis and biological evaluation of Combretastatin A-4 derivatives containing a 3’-O-substituted carbonic ether moiety as potential antitumor agents

“…CA-4 is recognized as an important parent compound, in terms of its biological effects, and hundreds of structural modified CA-4 derivatives have been synthesized and reported [15,16], where the modifications have traditionally been affected using either a Wittig reaction or a Perkin condensation reaction. Using the Wittig reaction, the CA-4 product is generally formed as a mixture with the corresponding trans isomer, which can be difficult to remove, and this can lead to complications in any follow-up work [17].…”

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

“…The rationale behind this is the significance of these moieties as privileged structures and the opportunity offered by them as anchors that could be harnessed for further diversification, besides they are present in number of antimitotic agents such as nocodazole and DF-203. 32,33 Moreover, the structural resemblance to E7010, a colchicine site binder (with crucial pyridine ring) was envisaged by the replacement of the olefinic bond by a pyridine ring to maintain the cis configuration. Such replacements of the olefinic bond with a ring system have been reported to provide potential advantage of promoting tubulin binding activity and tumor selectivity besides minimizing toxicity.…”

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

“…Compound (115) exhibits significant activity in ME-180 cell line with IC 50 value 4.01 mM that is comparable to the standard 5-flurouracil and also it is 10 fold less toxic to normal cell exhibiting an IC 50 value of 42.1 mM[150]. It is further reported the synthesis of combretastatin-amidobenzothiazole conjugates as anticancer agents.Compounds 116(a,b)have shown potent cytotoxicity against MCF-7 cells at 4 mM[151]. Substituted phenyl thiazolidinbenzo[d]thiazole-6-carboxylic acid derivatives synthesized and screened for their in vitro anticancer activity by MTT assay on human cervical cancer cell line (Hela) cell lines.…”