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Molecules 2012, 17(1), 873-883; doi:10.3390/molecules17010873

Novel Benzothiazole, Benzimidazole and Benzoxazole Derivatives as Potential Antitumor Agents: Synthesis and Preliminary in Vitro Biological Evaluation

State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medicinal School, Sichuan University, Chengdu 610041, Sichuan, China
These authors contributed equally to this work.
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Authors to whom correspondence should be addressed.
Received: 12 December 2011 / Revised: 6 January 2012 / Accepted: 10 January 2012 / Published: 17 January 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract

In a previous hit-to-lead research program targeting anticancer agents, two promising lead compounds, 1a and 1b, were found. However, the poor solubility of 1a and 1b made difficult further in vivo studies. To solve this problem, a lead optimization was conducted through introducing N-methyl-piperazine groups at the 2-position and 6-position. To our delight, the optimized analogue 1d showed comparable antiproliferative activity in vitro with better solubility, compared with 1a. Based on this result, the replacement of the benzothiazole scaffold with benzimidazole and benzoxazole moieties afforded 1f and 1g, whose activities were fundamentally retained. In the preliminary in vitro biological evaluation, the immunofluorescence staining of HCT116 cells indicated that 1d, 1f and 1g led to cytosolic vacuolization which was not induced by 1a at low micromolecular concentrations. These results suggest that these optimized compounds might potentially constitute a novel class of anticancer agents, which merit further studies.
Keywords: benzothiazole derivatives; benzimidazole; benzoxazole; antitumor; cytosolic vacuolization benzothiazole derivatives; benzimidazole; benzoxazole; antitumor; cytosolic vacuolization
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Xiang, P.; Zhou, T.; Wang, L.; Sun, C.-Y.; Hu, J.; Zhao, Y.-L.; Yang, L. Novel Benzothiazole, Benzimidazole and Benzoxazole Derivatives as Potential Antitumor Agents: Synthesis and Preliminary in Vitro Biological Evaluation. Molecules 2012, 17, 873-883.

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