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Mar. Drugs 2015, 13(4), 2488-2504; doi:10.3390/md13042488

Synthesis and in Vitro Antiproliferative Evaluation of Some B-norcholesteryl Benzimidazole and Benzothiazole Derivatives

1
College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001, China
2
Guangxi Key Laboratory of Beibu Gulf Marine Biodiversity Conservation, Qizhou University, Qizhou 535099, China
*
Author to whom correspondence should be addressed.
Academic Editor: Khalid El Sayed
Received: 29 January 2015 / Revised: 8 April 2015 / Accepted: 10 April 2015 / Published: 22 April 2015
View Full-Text   |   Download PDF [937 KB, uploaded 22 April 2015]   |  

Abstract

Taking orostanal (a compound from a Japanese marine sponge, Stelletta hiwasaensis) as a lead compound, some novel B-norcholesteryl benzimidazole and benzothiazole derivatives were synthesized. The antiproliferative activity of the compounds against human cervical carcinoma (HeLa), human lung carcinoma (A549), human liver carcinoma cells (HEPG2) and normal kidney epithelial cells (HEK293T) was assayed. The results revealed that the benzimidazole group was a better substituent than benzothiazole group for increasing the antiproliferative activity of compounds. 2-(3β′-Acetoxy-5β′-hydroxy-6′-B-norcholesteryl)benzimidazole (9b) with the structure of 6-benzimidazole displays the best antiproliferative activity to the cancer cells in all compounds, but is almost inactive to normal kidney epithelial cells (HEK293T). The assay of compound 9b to cancer cell apoptosis by flow cytometry showed that the compound was able to effectively induce cancer cell apoptosis. The research provided a theoretical reference for the exploration of new anti-cancer agents and may be useful for the design of novel chemotherapeutic drugs. View Full-Text
Keywords: cholesterol; B-norcholesteryl benzimidazoles; B-norcholesteryl benzothiazoles; antiproliferative activity; apoptosis cholesterol; B-norcholesteryl benzimidazoles; B-norcholesteryl benzothiazoles; antiproliferative activity; apoptosis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Cui, J.; Qi, B.; Gan, C.; Liu, Z.; Huang, H.; Lin, Q.; Zhao, D.; Huang, Y. Synthesis and in Vitro Antiproliferative Evaluation of Some B-norcholesteryl Benzimidazole and Benzothiazole Derivatives. Mar. Drugs 2015, 13, 2488-2504.

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