{"title":"作为具有潜在抗癌作用的细胞凋亡诱导剂的 2-(4-((1,3-二氧代异吲哚啉-2-基)甲基)苯基)-N-苯基噻唑-4-甲酰胺衍生物的合成与细胞毒性评估","authors":"Leila Hosseinzadeh, Ghazal Mahmoudi, Masoumeh Mahsa Mohammadi, Amin Hosseini, Hossein Malekshahi, Alireza Aliabadi","doi":"10.1134/S1068162024060062","DOIUrl":null,"url":null,"abstract":"<p><b>Objective:</b> Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. <b>Methods:</b> In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. <b>Results and Discussion:</b> Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (<b>VI</b>), (<b>VII</b>), (<b>VIII</b>), (<b>IX</b>), and (<b>XII</b>) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (<b>VII</b>) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (<b>VI–IX</b>), and (<b>XII</b>), just and just, 2-F derivative (<b>IV</b>) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. <b>Conclusions:</b> The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2095 - 2106"},"PeriodicalIF":1.1000,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects\",\"authors\":\"Leila Hosseinzadeh, Ghazal Mahmoudi, Masoumeh Mahsa Mohammadi, Amin Hosseini, Hossein Malekshahi, Alireza Aliabadi\",\"doi\":\"10.1134/S1068162024060062\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><b>Objective:</b> Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. <b>Methods:</b> In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. <b>Results and Discussion:</b> Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (<b>VI</b>), (<b>VII</b>), (<b>VIII</b>), (<b>IX</b>), and (<b>XII</b>) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (<b>VII</b>) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (<b>VI–IX</b>), and (<b>XII</b>), just and just, 2-F derivative (<b>IV</b>) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. <b>Conclusions:</b> The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer.</p>\",\"PeriodicalId\":758,\"journal\":{\"name\":\"Russian Journal of Bioorganic Chemistry\",\"volume\":\"50 6\",\"pages\":\"2095 - 2106\"},\"PeriodicalIF\":1.1000,\"publicationDate\":\"2024-12-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Russian Journal of Bioorganic Chemistry\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1134/S1068162024060062\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of Bioorganic Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1068162024060062","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects
Objective: Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. Methods: In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. Results and Discussion: Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (VI), (VII), (VIII), (IX), and (XII) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (VII) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (VI–IX), and (XII), just and just, 2-F derivative (IV) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. Conclusions: The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer.
期刊介绍:
Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.