{"title":"Emerging Claudin18.2-targeting Therapy for Systemic Treatment of Gastric Cancer: Seeking Nobility Amidst Danger.","authors":"Xueshuai Ye, Yongqiang Wu, Haiqiang Zhang","doi":"10.2174/0118715206329892240927081033","DOIUrl":"https://doi.org/10.2174/0118715206329892240927081033","url":null,"abstract":"<p><p>Gastric cancer in advanced stages lacked effective treatment options. claudin18.2 (CLDN18.2) is a membrane protein that is crucial for close junctions in the differentiated epithelial cells of the gastric mucosa, playing a vital role in barrier function, and can be hardly recognized by immune cells due to its polarity pattern. As the polarity of gastric tumor cells changes, claudin18.2 is exposed on the cell surface, resulting in immune system recognition, and making it an ideal target. In this review, we summarized the expression regulation mechanism of claudin18.2 both in normal cells and malignant tumor cells. Besides, we analyzed the available clinical results and potential areas for future research on claudin18.2-positive gastric cancer and claudin18.2-targeting therapy. In conclusion, claudin18.2 is an ideal target for gastric cancer treatment, and the claudin18.2-targeting therapy has changed the treatment pattern of gastric cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142370794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"MG132-mediated Suppression of the Ubiquitin-proteasome Pathway Enhances the Sensitivity of Endometrial Cancer Cells to Cisplatin.","authors":"Zhanhu Zhang, Yiqian Ding","doi":"10.2174/0118715206343550240919055701","DOIUrl":"https://doi.org/10.2174/0118715206343550240919055701","url":null,"abstract":"<p><strong>Background: </strong>Tumor cell resistance to cisplatin is a common challenge in endometrial cancer chemotherapy, stemming from various mechanisms. Targeted therapies using proteasome inhibitors, such as MG132, have been investigated to enhance cisplatin sensitivity, potentially offering a novel treatment approach.</p><p><strong>Objective: </strong>The aim of this study was to investigate the effects of MG132 on cisplatin sensitivity in the human endometrial cancer (EC) cell line RL95-2, focusing on cell proliferation, apoptosis, and cell signaling.</p><p><strong>Methods: </strong>Human endometrial cancer RL95-2 cells were exposed to MG132, and cell viability was assessed in a dose-dependent manner. The study evaluated the effect of MG132 on cisplatin-induced proliferation inhibition and apoptosis, correlating with caspase-3 activation and reactive oxygen species (ROS) upregulation. Additionally, we examined the inhibition of the ubiquitin-proteasome system and the expression of pro-inflammatory cytokines IL-1β, IL-6, IL-8, and IL-13 during MG132 and cisplatin co-administration.</p><p><strong>Results: </strong>MG132 exposure significantly reduced cell viability in a dose-dependent manner. It augmented cisplatin- induced proliferation inhibition and enhanced apoptosis, correlating with caspase-3 activation and ROS upregulation. Molecular analysis revealed a profound inhibition of the ubiquitin-proteasome system. MG132 also significantly increased the expression of cisplatin-induced pro-inflammatory cytokines, suggesting a transition from chronic to acute inflammation.</p><p><strong>Conclusion: </strong>MG132 enhances the therapeutic efficacy of cisplatin in human EC cells by suppressing the ubiquitin- proteasome pathway, reducing cell viability, enhancing apoptosis, and shifting the inflammatory response. These findings highlighted the potential of MG132 as an adjuvant in endometrial cancer chemotherapy. Further research is needed to explore detailed mechanisms and clinical applications of this combination therapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142360951","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Novel Quinoline Nitrate Derivatives: Synthesis, Characterization, and Evaluation of their Anticancer Activity with a Focus on Molecular Docking and NO Release.","authors":"Venkata Sowjanya Thanneeru, Naresh Panigrahi","doi":"10.2174/0118715206315415240830052608","DOIUrl":"https://doi.org/10.2174/0118715206315415240830052608","url":null,"abstract":"<p><strong>Background: </strong>Nitric Oxide (NO) has recently gained recognition as a promising approach in the field of cancer therapy. The quinoline scaffold is pivotal in cancer drug research and is known for its versatility and diverse mechanisms of action.</p><p><strong>Objective: </strong>This study presents the synthesis, characterization, and evaluation of novel quinoline nitrate derivatives as potential anticancer agents.</p><p><strong>Methods: </strong>The compounds were synthesized through a multi-step process involving the preparation of substituted 1-(2-aminophenyl) ethan-1-one, followed by the synthesis of substituted 2- (chloromethyl)-3,4-dimethylquinolines, and finally, the formation of substituted (3,4- dimethylquinolin-2-yl) methyl nitrate derivatives. The synthesized compounds were characterized using various spectroscopic techniques. Molecular docking studies were conducted to assess the binding affinity of the compounds to the EGFR tyrosine kinase domain.</p><p><strong>Results: </strong>The docking scores revealed varying degrees of binding affinity, with compound 6k exhibiting the highest score. The results suggested a correlation between molecular docking scores and anticancer activity. Further evaluations included MTT assays to determine the cytotoxicity of the compounds against Non-Small Cell Lung Cancer (A-549) and pancreatic cancer (PANC-1) cell lines. Compounds with electron-donating groups displayed notable anticancer potential, and there was a correlation between NO release and anticancer activity. The study also investigated nitric oxide release from the compounds, revealing compound 6g as the highest NO releaser.</p><p><strong>Conclusion: </strong>The synthesized quinoline nitrate derivatives showed promising anticancer activity, with compound 6g standing out as a potential lead compound. The correlation between molecular docking, NO release, and anticancer activity suggests the importance of specific structural features in the design of effective anticancer agents.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142360952","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Advancements in Pyrazine Derivatives as Anticancer Agents: A Comprehensive Review (2010-2024).","authors":"Mohammed Merae Alshahrani","doi":"10.2174/0118715206333399240912071555","DOIUrl":"https://doi.org/10.2174/0118715206333399240912071555","url":null,"abstract":"<p><p>Cancer, an intricate and formidable disease, continues to challenge Medical Science with its diverse manifestations and relentless progression. In the pursuit of novel therapeutic strategies, organic heterocyclic compounds have emerged as promising candidates due to their versatile chemical structures and intricate interactions with biological systems. Among these, pyrazine derivatives are characterized by a six-membered aromatic ring containing four carbon and two nitrogen atoms situated in a 1,4-orientation. These compounds garnered significant attention for their potential as anticancer agents. This comprehensive review provides a detailed analysis of the advancements made during this timeframe, encompassing the chemical diversity of pyrazine derivatives, their mechanisms of action at the cellular level, and structure-activity relationships, spanning the years 2010 to 2024. By examining their therapeutic potential, challenges, and future prospects, this review offers valuable insights into the evolving landscape of pyrazine derivatives as potent tools in the fight against cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142339474","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Preeti Kumari, Rakhi Mishra, Rupa Mazumder, Avijit Mazumder
{"title":"Acyl Urea Compounds Therapeutics and its Inhibition for Cancers in Women: A Review.","authors":"Preeti Kumari, Rakhi Mishra, Rupa Mazumder, Avijit Mazumder","doi":"10.2174/0118715206330232240913100744","DOIUrl":"https://doi.org/10.2174/0118715206330232240913100744","url":null,"abstract":"<p><p>Acyl urea compounds have garnered significant attention in cancer therapeutics, particularly for their potential effectiveness against cancers that predominantly affect women, such as breast and ovarian cancers. The paper presents a report on the investigation of acyl urea compounds that are reported to involve a multi-faceted approach, including synthetic chemistry, biological assays, and computational modeling. A wealth of information on acyl urea and its purported effects on cancer affecting women has been gathered from different sources and condensed to provide readers with a broad understanding of the role of acyl urea in combating cancer. Acylureas demonstrate promising results by selectively inhibiting key molecular targets associated with cancer progressions, such as EGFR, ALK, HER2, and the Wnt/β-catenin signaling pathway. Specifically, targeting acyl ureas impedes tumor proliferation and metastasis while minimizing harm to healthy tissues, offering a targeted therapeutic approach with reduced side effects compared to conventional chemotherapy. Continued research and clinical trials are imperative to optimize the efficacy and safety profiles of acylurea-based therapies and broaden their applicability across various cancer types. Acyl urea compounds represent a promising class of therapeutics for the treatment of cancers in women, particularly due to their ability to selectively inhibit key molecular targets involved in tumor growth and progression. The combination of synthetic optimization, biological evaluation, and computational modeling has facilitated the identification of several lead compounds with significant anticancer potential. This abstract explores the therapeutic mechanisms and targeted pathways of acyl ureas in combating these malignancies, which will be useful for future studies.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142339473","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Pioneering the Battle Against Breast Cancer: The Promise of New Bcl-2 Family.","authors":"Ali Farhang Boroujeni, Zeynep Ates-Alagoz","doi":"10.2174/0118715206320224240910054728","DOIUrl":"https://doi.org/10.2174/0118715206320224240910054728","url":null,"abstract":"<p><p>Currently, breast cancer is the most common cancer type, accounting for 1 in every 4 cancer cases. Leading both in mortality and incidence, breast cancer causes 1 in 4 cancer deaths. To decrease the burden of breast cancer, novel therapeutic agents which target the key hallmarks of cancer, are being explored. The Bcl-2 family of proteins has a crucial role in governing cell death, making them an attractive target for cancer therapy. As cancer chemotherapies lead to oncogenic stress, cancer cells upregulate the Bcl-2 family to overcome apoptosis, leading to failure of treatment. To fix this issue, Bcl-2 family inhibitors, which can cause cell death, have been introduced as novel therapeutic agents. Members of this group have shown promising results in in-vitro studies, and some are currently in clinical trials. In this review, we will investigate Bcl-2 family inhibitors, which are already in trials as monotherapy or combination therapy for breast cancer, and we will also highlight the result of in vitro studies of novel Bcl-2 family inhibitors on breast cancer cells. The findings of these studies have yielded encouraging outcomes regarding the identification of novel Bcl-2 family inhibitors. These compounds hold significant potential as efficacious agents for employment in both monotherapy and combination therapy settings.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142306980","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Rongfei Fang, Chunxiu Sha, Qun Xie, Min Yao, Dengfu Yao
{"title":"Alterations of Krüppel-like Factor Signaling and Potential Targeted Therapy for Hepatocellular Carcinoma.","authors":"Rongfei Fang, Chunxiu Sha, Qun Xie, Min Yao, Dengfu Yao","doi":"10.2174/0118715206301453240910044913","DOIUrl":"https://doi.org/10.2174/0118715206301453240910044913","url":null,"abstract":"<p><p>Krüppel-like factors (KLFs, total 18 members) from the zinc finger protein (ZFP) super-family have a wide range of biological functions in hepatocellular carcinoma (HCC). This paper reviews the recent some progresses of aberrant KLFs with their potential values for diagnosis, prognosis, and targeted therapy in HCC. The recent advances of oncogenic KLFs in the diagnosis, prognosis, and targeted therapy of HCC were reviewed based on the related literature on PUBMED and clinical investigation. Based on the recent literature, KLFs, according to biological functions in HCC, are divided into 4 subgroups: promoting (KLF5, 7, 8, 13), inhibiting (KLF3, 4, 9~12, 14,17), dual (KLF2,6), and unknown functions (KLF1, 15, 16, or 18 ?). HCC-related KLFs regulate downstream gene transcription during hepatocyte malignant transformation, participating in cell proliferation, apoptosis, invasion, and metastasis. Some KLFs have diagnostic or prognostic value, and other KLFs with inhibiting promoting function or over-expressing inhibiting roles might be molecular targets for HCC therapy. These data have suggested that Abnormal expressions of KLFs were associated with HCC progression. Among them, some KLFs have revealed the clinical values of diagnosis or prognosis, and other KLFs with the biological functions of promotion or inhibition might be as effectively molecular targets for HCC therapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142306979","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Rafat Milad Mohareb, Mahmoud Ali Abdelaziz, Rasha Jame, Noha Omer, Hanan Maged Labib
{"title":"Synthesis of New Chromen-5-one Derivatives from Dimedone and their Antiproliferative Evaluations against Selected Cancer Cell Lines Together with Hepatocellular Carcinoma and Cervical Carcinoma.","authors":"Rafat Milad Mohareb, Mahmoud Ali Abdelaziz, Rasha Jame, Noha Omer, Hanan Maged Labib","doi":"10.2174/0118715206323592240909101754","DOIUrl":"https://doi.org/10.2174/0118715206323592240909101754","url":null,"abstract":"<p><strong>Background: </strong>The coumarin nuclei, which exist in many heterocyclic compounds, has gained a lot of attention over the past decade due to their wide range of biological activities such as antibacterial, anticoagulant, antiviral, antifungal, anticancer, and anti-inflammatory properties.</p><p><strong>Objective: </strong>The multi-component reactions of 5,5-dimethylcyclohexane-1,3-dione with acetophenone derivatives and triethoxymethane produced biologically active target chromene molecules and their fused derivatives.</p><p><strong>Methods: </strong>The reaction of 5,5-dimethylcyclohexane-1,3-dione and each of triethoxymethane and acetophenone derivatives 3a-g in absolute ethanol containing triethylamine gave the 4,6,7,8-tetrahydro-5H-chromen-5-one derivatives 4a-g. Compounds 4a-d were used for further heterocyclization reactions to produce biologically active fused pyrazole, thiophene, and thiazole derivative corporate with the chromenes caffold.</p><p><strong>Results: </strong>The cytotoxicity of the synthesized compounds were evaluated using six cancer cell lines together with c-Met kinase and PC-3 cell line inhibitions. In addition, cytotoxicity toward hepatocellular carcinoma HepG2 and cervical carcinoma HeLa was carried out as well as the in-vitro cytotoxic potential for all compounds against peripheral blood lymphocytes (PBL) extracted from healthy donors. Morphological changes of the A549 cell line by the two most active compounds were also studied.</p><p><strong>Conclusion: </strong>The synthesized heterocyclic compounds were originally obtained from 5,5-dimethylcyclohexane1,3-dione. Several of the produced compounds exhibited high inhibitions toward several cancer cell lines proving high inhibitions, therefore, encouraging further studies to synthesize heterocyclic compounds based on chromene scaffold.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142279368","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Esther Ugo Alum, Tabussam Tufail, Daniel Ejim Uti, Patrick Maduabuchi Aja, Christian Emeka Offor, Udu Ama Ibiam, Chris U A Ukaidi, Benedict Nnachi Alum
{"title":"Utilizing Indigenous Flora in East Africa for Breast Cancer Treatment: An Overview.","authors":"Esther Ugo Alum, Tabussam Tufail, Daniel Ejim Uti, Patrick Maduabuchi Aja, Christian Emeka Offor, Udu Ama Ibiam, Chris U A Ukaidi, Benedict Nnachi Alum","doi":"10.2174/0118715206338557240909081833","DOIUrl":"https://doi.org/10.2174/0118715206338557240909081833","url":null,"abstract":"<p><strong>Background: </strong>Breast cancer is a significant global health challenge, contributing substantially to cancer- related deaths. Conventional treatment methods, including hormone therapy, chemotherapy, surgical interventions, and radiation, have long been utilized. However, these traditional treatments are often associated with serious side effects and drug resistance, limiting their efficacy.</p><p><strong>Aim: </strong>This review aims to explore the potential of medicinal plants used in breast cancer management in East Africa, focusing on their bioactive compounds and anticancer properties.</p><p><strong>Methods: </strong>A comprehensive literature search was conducted to examine the effectiveness of medicinal plants in treating breast cancer across Kenya, Ethiopia, Uganda, Tanzania, and Rwanda. Relevant studies published between 2003 and 2023 were identified using keywords related to breast cancer and medicinal plants. The search was performed across multiple databases, including Google Scholar, PubMed, Scopus, Web of Science Core Collection, and Science Direct.</p><p><strong>Results: </strong>Numerous natural compounds found in East African medicinal plants including Cymbopogon citratus (Lemongrass,) Tabebuia avellanedae, Prunus africana (African Cherry), Euclea divinorum, Berberis holstii, Withania somnifera (Ashwagandha, Curcuma longa (Turmeric), Garcinia mangostana (Mangosteen, Vitis vinifera (Grapevine), Eugenia jambolana (Java Plum), Moringa oleifera (Drumstick Tree), Camellia sinensis (Tea), Glycine max (Soybean), Catharanthus roseus, Madagascar Periwinkle), Rhus vulgaris (Wild Currant) exhibit significant anticancer properties. These compounds have demonstrated the ability to reduce breast cancer aggressiveness, inhibit cancer cell proliferation, and modulate cancer-related pathways. Current research focuses on these natural and dietary compounds to develop more effective strategies for treating breast cancer.</p><p><strong>Conclusion: </strong>The findings suggested that East African medicinal plants hold promise as complementary treatments for breast cancer, offering potential benefits such as affordability, cultural appropriateness, and sustainability. Further research into these plants and their bioactive compounds could revolutionize breast cancer treatment, improving survival rates and addressing the rising incidence of breast cancer-related fatalities. Other: The review underscores the importance of continued research, conservation, and the integration of ancient healing methods to fully harness the potential of East African flora in breast cancer management.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142279369","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Exploring Tryptophan-based Short Peptides: Promising Candidate for Anticancer and Antimicrobial Therapies.","authors":"Neha Rai, Richa Tripathy Tiwari, Adarsh Sahu, Ekta Verma, Swati Rathore, Shailendra Patil, Asmita Gajbhiye Patil","doi":"10.2174/0118715206260662240613054521","DOIUrl":"https://doi.org/10.2174/0118715206260662240613054521","url":null,"abstract":"<p><strong>Background: </strong>Ultra-short peptides are essential therapeutic agents due to their heightened selectivity and reduced toxicity. Scientific literature documents the utilization of dipeptides, tripeptides, and tetrapeptides as promising agents for combating cancer. We have created a range of tryptophan-based peptides derived from literature sources in order to assess their potential as anticancer drugs.</p><p><strong>Methods: </strong>We present the results of our study on the antibacterial and anticancer effectiveness of 10 ultra-short peptides that were produced utilizing microwave-assisted solid phase peptide synthesis. The synthesized peptides underwent screening for in vitro antibacterial activity using the agar dilution method.</p><p><strong>Results: </strong>HPLC, LC-MS, 1H NMR, and 13C NMR spectroscopy were used to analyze the synthesized peptides. In tests using the HeLa and MCF-7 cell lines, the synthesized peptides' anticancer efficacy was assessed. The study found that two peptides showed potential median inhibitory concentration (IC50) values of 3.9±0.13 μM and 1.8±0.09 μM, respectively, and showed more activity than the reference medication doxorubicin.</p><p><strong>Conclusion: </strong>The antibacterial activity of synthesized peptides 3b and 4b was found to be better than the other synthetic peptides. MIC value of roughly 5-50 μg/mL for peptides 3a, 4c, and 4d showed strong antifungal activity against Candida albicans. The synthesized peptides were also evaluated for their anticancer activity against HeLa and MCF-7 cell lines, and found that peptides 3e and 4e were more potent than other peptides against doxorubicin.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":2.6,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142279367","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}