Design, synthesis, and evaluation of novel combretastatin A‐4 based chalcone derivatives as anticancer agents,Journal of Heterocyclic Chemistry

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Design, synthesis, and evaluation of novel combretastatin A‐4 based chalcone derivatives as anticancer agents
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-11-16 , DOI: 10.1002/jhet.4186
Bethi Rathnakar ₁ , Gajula S. Kumar ₁ , Saleem P. Mahammad ₁ , Sridhar Gattu ₂ , Sambaru Kalyani ₃ , Rameshwar Nimma ₁ , Mavurapu Satyanarayana ₁

Affiliation

A series of combretastatin A‐4 based chalcones (14a‐l) were designed, synthesized and these compounds examined for inhibitory effects on the proliferation of human lung (A549), breast (MCF‐7), melanoma (A375), and colon (HT‐29) carcinoma cells. Compounds 14b, 14c, 14e, 14h, and 14i (tri/dimethoxy, methyl, and mono/dinitro derivatives) have exhibited the most potent antiproliferative activity with IC₅₀ < 2 μM and the hexa methoxy derivative 14b, the most promising one, which displayed the potent inhibitory activities in MCF‐7 (IC₅₀: 10 nM), A375 (IC₅₀: 12 nM), and A549 (IC₅₀: 65 nM) cell lines, and is 18 times more potent than the CA‐4. Compound 14b represents a new scaffold and the results provide insights into further development of anticancer agents.

中文翻译：

设计，合成和评估基于康普他汀A-4的新型查尔酮衍生物作为抗癌药

设计，合成了一系列基于康维他汀A-4的查耳酮（14a-1），并检查了这些化合物对人肺（A549），乳腺癌（MCF-7），黑素瘤（A375）和结肠（ HT‐29）癌细胞。化合物14b，14c，14e，14h和14i（三/二甲氧基，甲基和单/二硝基衍生物）表现出最强的抗增殖活性，IC ₅₀ <2μM ，最有前途的六甲氧基衍生物14b在MCF-7（IC显示强效抑制活性₅₀，A375（IC：10nm）的₅₀：12纳米）和A549（IC₅₀：65 nM）的细胞系，并且是18倍，比CA-4更有效。化合物14b代表了一种新的支架，其结果为进一步开发抗癌药物提供了见识。

更新日期：2020-11-16

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