Design, synthesis and anticancer evaluation of substituted aryl-1,3-oxazole incorporated pyrazole-thiazole derivatives

IF 2.218 Q2 Chemistry Chemical Data Collections Pub Date : 2024-03-01 DOI:10.1016/j.cdc.2024.101127

P. Venkata Ramana Reddy , E. Shivakumar , Dittakavi Ramachandran

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Abstract

A new library of different types of aryl ring attached pyrazole-thiazole-oxazoles (11a-j) was prepared and their structures were characterized by ¹HNMR, ¹³CNMR and mass spectral data. Further, these compounds were evaluated for anticancer effects towards a panel of four human cancer cell lines including SiHa (cervix cancer), A549 (lung cancer), MCF-7 (breast cancer) and Colo-205 (colon cancer) by the MTT method, with etoposide used as a reference drug. Most of the tested compounds exhibited good anticancer activity with IC₅₀ values ranging from 0.13±0.046 µM to 18.6 ± 6.34 µM and the reference drug showed values ranging from 0.14 ± 0.017 µM to 3.11±0.11 µM, respectively. Among these compounds 11e, 11f, 11 g and 11 h displayed more potent anticancer activity as etoposide. All compounds showed selective cytotoxicity against cancer cells but not against normal Vero cells (IC₅₀ = >24 µM), justifying the designing approach to develop a selective anticancer agent.

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作为抗癌剂的取代芳基-1,3-恶唑并入吡唑-噻唑衍生物的设计、合成和抗癌评估

制备了一个新的不同类型芳基环连接吡唑-噻唑-噁唑（11a-j）化合物库，并通过 1HNMR、13CNMR 和质谱数据对其结构进行了表征。此外，还采用 MTT 法评估了这些化合物对四种人类癌细胞株（包括 SiHa（宫颈癌）、A549（肺癌）、MCF-7（乳腺癌）和 Colo-205（结肠癌））的抗癌效果，并以依托泊苷作为参照药物。大多数受试化合物都表现出良好的抗癌活性，IC50 值从 0.13±0.046 µM 到 18.6 ± 6.34 µM，参比药物的 IC50 值从 0.14 ± 0.017 µM 到 3.11±0.11 µM。在这些化合物中，11e、11f、11 g 和 11 h 与依托泊苷相比具有更强的抗癌活性。所有化合物对癌细胞都显示出选择性细胞毒性，但对正常 Vero 细胞却没有（IC50 = >24 µM），这证明了开发选择性抗癌剂的设计方法是正确的。

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来源期刊

Chemical Data Collections Chemistry-Chemistry (all)

CiteScore

6.10

自引率

0.00%

发文量

169

审稿时长

24 days

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