21 February 2013 Novel 2DG-based harmine derivatives for targeted cancer therapy
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Proceedings Volume 8582, Biophotonics and Immune Responses VIII; 85820V (2013) https://doi.org/10.1117/12.2003268
Event: SPIE BiOS, 2013, San Francisco, California, United States
Harmine is a beta-carboline alkaloid from the plant Peganum harmala. These alkaloids were stimulated by their promising antitumor activities in the recent years. In this study, we designed and synthesized two harmine derivatives #1and #2 modified at position-9 of harmine with ethyl and phenylpropyl, respectively. To improve the tumor targeting capability, #1’ and #2’ were synthesized by conjugating 2-amino-2-deoxy-D-glucose (2DG) to the derivatives #1 and #2, respectively. The MTT assays of all these compounds in vitro against L02, HepG2 showed all compounds had low toxicity to normal cells (L02) and significantly enhanced carcinoma cell inhibitory rate compared to harmine. Cytotoxicity against liver cancer cell lines of compound #1’ #2’ is higher than #1 #2, and even the compound #2’ is better than positive drug 5-FU. The compound #2’, a novel 2DG-based harmine derivatives, could become a promising drug for targeted cancer therapy and combination therapy with other antitumor drugs.
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Aqin Wang, Aqin Wang, Yuqi Chen, Yuqi Chen, Wei R. Chen, Wei R. Chen, Yueqing Gu, Yueqing Gu, "Novel 2DG-based harmine derivatives for targeted cancer therapy", Proc. SPIE 8582, Biophotonics and Immune Responses VIII, 85820V (21 February 2013); doi: 10.1117/12.2003268; https://doi.org/10.1117/12.2003268

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