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Design, Synthesis and In‐Vitro Antitumor Activity of Lupeol Derivatives via Modification at C‐3 and C‐30 Positions
ChemistrySelect ( IF 1.9 ) Pub Date : 2019-02-06 , DOI: 10.1002/slct.201803101 Monika Saini 1 , Mohammad Faheem Khan 2 , Reetu Sangwan 1 , Mohsin Ali Khan 2 , Ashok Kumar 3 , Ruchi Verma 1 , Tanveer Ahamad 2 , Sudha Jain 1
ChemistrySelect ( IF 1.9 ) Pub Date : 2019-02-06 , DOI: 10.1002/slct.201803101 Monika Saini 1 , Mohammad Faheem Khan 2 , Reetu Sangwan 1 , Mohsin Ali Khan 2 , Ashok Kumar 3 , Ruchi Verma 1 , Tanveer Ahamad 2 , Sudha Jain 1
Affiliation
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Lupeol has been isolated from ethanol extract of stem bark of Bombax ceiba through normal phase column chromatography. Total fourteen derivatives of lupeol were synthesized and assayed for in vitro antitumor activities against MDA MB‐231, HeLa and A549 cell lines. In cell proliferation experiments, pyrimidine‐2(5H)‐thione derivative (15) was found to be most potent and significantly inhibited all three tested cancer cell lines i. e. MDA MB‐231 (IC50 27.13±2.13), HeLa (IC50 45.95±1.42) and A549 (IC50 46.27±0.9). The (2, 4‐dinitrophenyl) hydrazyl‐3‐lupeol Derivative (12) exhibited antitumor activity against MDA MB‐231 (IC50 35.88±1.9) and HeLa cells (IC50 31.91±1.6) whereas (2, 4‐dinitrophenyl)‐2H‐imidazole derivative (14) showed activity against MDA MB‐231 (IC50 38.05±1.9) and A549 (IC50 42.01±0.90) cells respectively. Structure activity relationship is also described. Our study showed that compound 15 exhibited promising activity against MDA MB‐231 and A549 cancer cell lines.
中文翻译：
通过在C-3和C-30位置进行修饰，对Lupeol衍生物进行设计，合成和体外抗肿瘤活性
羽扇豆醇已从的茎皮的乙醇提取物中分离木棉通过正相柱色谱。合成了总共14种羽扇豆酚衍生物，并测定了其对MDA MB‐231，HeLa和A549细胞系的体外抗肿瘤活性。在细胞增殖实验中，发现嘧啶-2（5H）-硫酮衍生物（15）最有效并且显着抑制了所有三种测试的癌细胞系。e。MDA MB‐231（IC 50 27.13±2.13），HeLa（IC 50 45.95±1.42）和A549（IC 50 46.27±0.9）。（2，4-二硝基苯基）肼基3-lupeol衍生物（12）对MDA MB-231具有抗肿瘤活性（IC 5035.88±1.9）和HeLa细胞（IC 50 31.91±1.6），而（2，4-二硝基苯基）-2H-咪唑衍生物（14）显示出对MDA MB‐231（IC 50 38.05±1.9）和A549（IC 50 42.01 ）的活性±0.90）个单元格。还描述了结构活性关系。我们的研究表明，化合物15对MDA MB‐231和A549癌细胞具有良好的活性。
更新日期：2019-02-06
中文翻译：
通过在C-3和C-30位置进行修饰，对Lupeol衍生物进行设计，合成和体外抗肿瘤活性
羽扇豆醇已从的茎皮的乙醇提取物中分离木棉通过正相柱色谱。合成了总共14种羽扇豆酚衍生物，并测定了其对MDA MB‐231，HeLa和A549细胞系的体外抗肿瘤活性。在细胞增殖实验中，发现嘧啶-2（5H）-硫酮衍生物（15）最有效并且显着抑制了所有三种测试的癌细胞系。e。MDA MB‐231（IC 50 27.13±2.13），HeLa（IC 50 45.95±1.42）和A549（IC 50 46.27±0.9）。（2，4-二硝基苯基）肼基3-lupeol衍生物（12）对MDA MB-231具有抗肿瘤活性（IC 5035.88±1.9）和HeLa细胞（IC 50 31.91±1.6），而（2，4-二硝基苯基）-2H-咪唑衍生物（14）显示出对MDA MB‐231（IC 50 38.05±1.9）和A549（IC 50 42.01 ）的活性±0.90）个单元格。还描述了结构活性关系。我们的研究表明，化合物15对MDA MB‐231和A549癌细胞具有良好的活性。
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