吡啶-咪唑[1,2-a]吡嗪-恶唑芳基酰胺类抗癌药物的合成及生物学评价

IF 2.218 Q2 Chemistry

Chemical Data Collections Pub Date : 2025-02-01 DOI:10.1016/j.cdc.2024.101176

Narendhar Reddy Vanam , Prakash Gadipelli , Jaya Shree Anireddy

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引用次数: 0

摘要

以依托泊苷（etoposide, etoposide）为标准药物，设计、合成了一系列新的吡啶-咪唑[1,2- A]吡嗪-恶唑（15a-j）芳基酰胺衍生物，并对MCF-7（人乳腺癌）、A549（人肺癌）、Colo-205（人结肠癌）和A2780（人卵巢癌）细胞系进行了MTT还原实验，筛选了它们的抗癌活性。在所合成的衍生物中，含三甲氧基给电子取代基的化合物15a对MCF-7、A549、Colo-205和A2780细胞株具有较强的抗癌活性，IC50值为0.03±0.0043µM；0.02±0.0077µm；0.12±0.066µm；和0.17±0.059µM。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Synthesis and biological evaluation of aryl amide derivatives of pyridine-imidazo[1,2-a]pyrazine-oxazole as anticancer agents

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Synthesis and biological evaluation of aryl amide derivatives of pyridine-imidazo[1,2-a]pyrazine-oxazole as anticancer agents

A new series of aryl amide derivatives of pyridine-imidazo[1,2-a]pyrazine-oxazoles (15a-j) has been designed, synthesized and screened for their anticancer activity against MCF-7 (human breast cancer), A549 (human lung cancer), Colo-205 (human colon cancer) and A2780 (human ovarian cancer) cell lines by using MTT reduction assay protocol with etoposide (Etoposide) as standard drug. Among the synthesized derivatives, the compound 15a with trimethoxy electron donating substituent showed potent anticancer activity against MCF-7, A549, Colo-205, and A2780 cell lines with IC₅₀ values of 0.03 ± 0.0043 µM; 0.02 ± 0.0077 µM; 0.12 ± 0.066 µM; and 0.17 ± 0.059 µM respectively.

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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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