Abstract
Novel imidazole derivatives were designed, prepared, and evaluated in vitro for antitumor activity. The majority of the tested derivatives showed improved antiproliferative activity compared to the positive control drugs 5-FU and MTX. Among them, compound 4f exhibited outstanding antiproliferative activity against three cancer cell lines and was considerably more potent than both 5-FU and MTX. In particular, the selectivity index indicated that the tolerance of normal L-02 cells to 4f was 23–46-fold higher than that of tumor cells. This selectivity was significantly higher than that exhibited by the positive control drugs. Furthermore, compound 4f induced cell apoptosis by increasing the protein expression levels of Bax and decreasing those of Bcl-2 in a time-dependent manner. Therefore, 4f could be a potential candidate for the development of a novel antitumor agent.
Highlights
The essential hallmarks of cancer include an altered cancer–cell intrinsic metabolism, i.e., tumor cell metabolism, which was seen as cancer’s Achilles heel [1]
We reported a series of imidazole-fused quinoline compound I and we found that compound antitumor activity in vitro
We explored the structure–anticancer anticancer activity and antitumor mechanisms of from thesethe compounds the activity relationships andrelationships antitumor mechanisms of these compounds perspectivefrom of apoptosis
Summary
The essential hallmarks of cancer include an altered cancer–cell intrinsic metabolism, i.e., tumor cell metabolism, which was seen as cancer’s Achilles heel [1]. The antitumor potency of Tanshinone-IIA has been enhanced pharmacophore, displaces recombinant p53 protein from its complex with MDM2 and selectively by the introduction of an imidazole moiety (Figure 1, TA12) in order to block cancer cell invasion inhibits MDM2-p53 interaction both in vitro and in vivo [15]. Using compound II as a lead, we designed and synthesized activities were not strong enough as a potent antitumor agent.and. The effects of LogP and weredesigned considered, and several aliphatic and aromatic amines were selected and linked to the 1-phenyl hydrogen bonds on bioavailability were considered, and several aliphatic and aromatic amines were imidazole scaffold using a succinyl group as a cross-linker. 1-(4-substituted phenyl)-2-ethyl imidazole derivatives exhibited excellent antitumor activity. Imidazole derivatives that that exhibited excellent antitumor activity.
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