噻唑烷-2,4-二联苯衍生物抗癌剂的设计、合成及生物学评价。

Q2 Medicine Asian Pacific Journal of Cancer Prevention Pub Date : 2025-01-01 DOI:10.31557/APJCP.2025.26.1.101

Udaya Sri Earati, Kiran Gangarapu, Mahendar Porika

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引用次数: 0

摘要

目的：设计并合成新的噻唑烷-2,4-二酮-联苯衍生物（10a-j）文库。所有化合物都用光谱数据进行了表征。此外，还对它们的体外抗癌活性进行了评估。方法：按照Scheme-1计划合成化合物，并采用MTT法对宫颈癌（Hela）、前列腺癌（PC3）、肺癌细胞和乳腺癌（MDA-MB-231） 4种人癌细胞进行筛选。阳性对照选用阿霉素。结果：大部分化合物具有中至良好的活性。其中，化合物10b和10d和表现出较强的活性。其中一种化合物10d显示出显著的抗癌活性。与EGFR靶标（PDB ID: 1M17）的分子对接研究表明，化合物10b和10d与相同的残基表现出良好的分子相互作用，类似于共晶配体厄洛替尼。结论：这两种化合物都能很好地靶向EGFR活性位点，并表现出较强的抑制作用。

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Design, Synthesis and Biological Evaluation of Thiazolidine-2,4-dione-biphenyl Derivatives as Anticancer Agents.

Objective: A new library of Thiazolidine-2,4-dione-biphenyl Derivatives derivatives (10a-j) was designed and synthesized. All compounds were characterized by spectral data. Further, these were evaluated for their in vitro anticancer activity.

Methods: The compounds were synthesized as planned in the Scheme-1 and compounds were screened against four human cancer cell lines like cervical cancer (Hela), prostate cancer (PC3), lung cancer cells and breast cancer cells (MDA-MB-231) by employing of MTT assay. Doxorubicin was chosen as positive control.

Result: Most of the compounds showed moderate to good activity. Among them, these compounds 10b and 10d and displayed more potent activity. Predominantly, one compound 10d showed remarkable anticancer activity. Molecular docking studies with EGFR target (PDB ID: 1M17) exhibits compounds 10b and 10d showed desirable molecular interactions with the same residue similar to cocrystal ligand Erlotinib.

Conclusion: This results indicate that these two compounds are well targeted the EGFR active sites and showed more inhibitory effects than the other compounds.

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来源期刊

Asian Pacific Journal of Cancer Prevention 医学-肿瘤学

CiteScore

2.80

自引率

0.00%

发文量

779

审稿时长

3 months

期刊介绍： Cancer is a very complex disease. While many aspects of carcinoge-nesis and oncogenesis are known, cancer control and prevention at the community level is however still in its infancy. Much more work needs to be done and many more steps need to be taken before effective strategies are developed. The multidisciplinary approaches and efforts to understand and control cancer in an effective and efficient manner, require highly trained scientists in all branches of the cancer sciences, from cellular and molecular aspects to patient care and palliation. The Asia Pacific Organization for Cancer Prevention (APOCP) and its official publication, the Asia Pacific Journal of Cancer Prevention (APJCP), have served the community of cancer scientists very well and intends to continue to serve in this capacity to the best of its abilities. One of the objectives of the APOCP is to provide all relevant and current scientific information on the whole spectrum of cancer sciences. They aim to do this by providing a forum for communication and propagation of original and innovative research findings that have relevance to understanding the etiology, progression, treatment, and survival of patients, through their journal. The APJCP with its distinguished, diverse, and Asia-wide team of editors, reviewers, and readers, ensure the highest standards of research communication within the cancer sciences community across Asia as well as globally. The APJCP publishes original research results under the following categories: -Epidemiology, detection and screening. -Cellular research and bio-markers. -Identification of bio-targets and agents with novel mechanisms of action. -Optimal clinical use of existing anti-cancer agents, including combination therapies. -Radiation and surgery. -Palliative care. -Patient adherence, quality of life, satisfaction. -Health economic evaluations.