التفاصيل البيبلوغرافية
| العنوان: |
Design and Synthesis of Thiourea-Conjugating Organic Arsenic D-Glucose with Anticancer Activities. |
| المؤلفون: |
Fu, Boqiao, Liu, Wenxuan, Wang, Yufeng, Li, Guorui, Wang, Yingsha, Huang, Xinyuan, Shi, Hongan, Qin, Caiqin |
| المصدر: |
Molecules; Jun2024, Vol. 29 Issue 12, p2850, 10p |
| مستخلص: |
Organic arsenic compounds such as p-aminophenylarsine oxide (p-APAO) are easier for structural optimization to improve drug-like properties such as pharmacokinetic properties, therapeutic efficacy, and target selectivity. In order to strengthen the selectivity of 4-(1,3,2-dithiarsinan-2-yl) aniline 7 to tumor cell, a thiourea moiety was used to strengthen the anticancer activity. To avoid forming a mixture of α/β anomers, the strategy of 2-acetyl's neighboring group participation was used to lock the configuration of 2,3,4,6-tetra-O-acetyl-β-d-glucopyranosyl isothiocyanate from 2,3,4,6-tetra-O-acetyl-α-d-glucopyranosyl bromide. 1-(4-(1,3,2-dithiarsinan-2-yl) aniline)-2-N-(2,3,4,6-tetra-O-acetyl-β-d-glucopyranos-1-yl)-thiourea 2 can increase the selectivity of human colon cancer cells HCT-116 (0.82 ± 0.06 μM vs. 1.82 ± 0.07 μM) to human embryonic kidney 293T cells (1.38 ± 0.01 μM vs. 1.22 ± 0.06 μM) from 0.67 to 1.68, suggesting a feasible approach to improve the therapeutic index of arsenic-containing compounds as chemotherapeutic agents. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
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