原：CURRENT MEDICINAL CHEMISTRY - ANTI-CANCER AGENTS由该领域的领导者撰写的深入评论和客座编辑的问题，涵盖了癌症药物化学的一系列当前主题。该杂志只考虑发表高质量的研究论文。ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY 是每一位希望随时了解癌症药物发现最新和最重要进展的药物化学家的重要期刊。

Anti-Cancer Agents in Medicinal Chemistry is a journal authored by leaders in the field, offering in-depth reviews and guest-edited issues that cover a range of current topics in cancer medicinal chemistry. The journal only considers high-quality research papers for publication, making it an essential resource for medicinal chemists who wish to stay informed about the latest and most significant advancements in cancer drug discovery.

《Anti-Cancer Agents in Medicinal Chemistry》是一本由该领域的领导者撰写的期刊，提供深入的评论和特邀编辑的专题，涵盖癌症药物化学的多个当前主题。该杂志只考虑发表高质量的研究论文，是每位希望了解癌症药物发现最新进展的药物化学家的重要参考。

Anti-Cancer Agents in Medicinal Chemistry

Dinesh Kumar Mehta

Rina Das

Anti-cancer agents in medicinal chemistry

Anticancer Agents Med Chem

Current Expansions and Future Perspectives in Anticancer Drug Therapy.

抗癌药物治疗的现状扩展与未来展望

Reactive Oxygen Species (ROS) refers to the highly reactive substances which contain oxygen radicals. Hypochlorous acid, peroxides, superoxide, singlet oxygen, alpha-oxygen, and hydroxyl radicals are the major examples of ROS. Generally, the reduction of oxygen (O2) in molecular form produces superoxide (•O2 -) anion. ROS are produced during a variety of biochemical reactions within the cell organelles, such as endoplasmic reticulum, mitochondria, and peroxisome. Naturally, ROS are also formed as a byproduct of the normal metabolism of oxygen. The production of ROS can be induced by various factors such as heavy metals, tobacco, smoke, drugs, xenobiotics, pollutants, and radiation. From various experimental studies, it is reported that ROS acts as either a tumor-suppressing or a tumor-promoting agent. The elevated level of ROS can arrest the growth of tumors through the persistent increase in cell cycle inhibition. The increased level of ROS can induce apoptosis by both intrinsic and extrinsic pathways. ROS is considered to be a tumor-suppressing agent as the production of ROS is due to the use of most of the chemotherapeutic agents in order to activate cell death. The cytotoxic effect of ROS provides impetus towards apoptosis, but in higher levels, ROS can cause initiation of malignancy that leads to uncontrolled cell death in cancer cells. In contrast, some species of ROS can influence various activities at the cellular level, including cell proliferation. This review highlights the genesis of ROS within cells by various routes and their role in cancer therapies.

Biswa Mohan Sahoo

Bimal Krishna Banik

Preetismita Borah

Adya Jain

Reactive Oxygen Species (ROS): Key Components in Cancer Therapies

活性氧(ROS): 癌症治疗的关键成分

The present application reports a series of novel Arcyriaflavin-A derivatives as PIM kinase inhibitors for the effective treatment of cancer. The application also describes the synthesis of compounds in detail, use, pharmaceutical composition, pharmaceutically acceptable salts, and treatment.

Surya K. De

Novel Arcyriaflavin-A Derivatives as PIM Kinase Inhibitors for Treating Cancer

新型阿日菌素A衍生物作为治疗癌症的PIM激酶抑制剂

Background: As the number of new cancer cases increases every year, there is a necessity to develop new drugs for the treatment of different types of cancers. Plants' resources are considered to be huge reservoirs for therapeutic agents in nature. Among all the medicinal plants, Oroxylum indicum is one of the most widely used medicinal plants in India, China, and Southeast Asian countries. Combinatorial drug treatment, on the other hand, is favored over single drug treatment in order to target multiple biomolecular moieties that help in the growth and development of cancer. Therefore, combinatorial drug treatment using a co-crystal of multiple drugs gives researchers an idea of the development of a new type of drug for targeting multiple targets. In this study, a new co-crystal of chrysin and oroxylin A was isolated from the leaves of O. indicum, and its anticancer properties were studied in cervical cancer cells HeLa. Aim: This study was conducted with the aim of identifying new anticancer compounds from the leaves of Oroxylum indicum and studying the anticancer properties of the isolated compound. Objective: In this study, we elucidated the structure of a new co-crystal compound, which was isolated from the leaf extract of Oroxylum indicum. The apoptosis induction mechanism of the newly discovered co-crystal in HeLa cells was also studied. Methods: A crystal compound from the chloroform extract of leaves of Oroxylum Indicum was isolated by solvent fractionation and chromatographic methods involving HPLC. The molecular structure of the isolated crystal was elucidated by Single Crystal-XRD, FT-IR analysis, and further determined by LC-MS. The antiproliferative activity was carried out using an MTT assay and fluorescence microscopy, and the mechanism of apoptosis was determined using Western blotting techniques. Results: The novel co-crystal consists of two active pharmaceutical ingredients (APIs) in a 1:1 ratio, i.e., oroxylin A and chrysin. The isolated new co-crystal induced death in HeLa cells with a very low IC50 value of 8.49μM. It induced caspase-dependent apoptosis in HeLa cells by activation of Caspase-3 through inhibition of ERKs and activation of p38 of MAPK cell signalling pathway. Conclusion: This study presents the first report on the discovery of a naturally occurring co-crystal of chrysin and oroxylin A and the involvement of ERKs and p38 of MAPK pathways in the induction of apoptosis in HeLa cells by the co-crystal. Our study sheds light on the development of a co-crystal of chrysin and oroxylin A in a specific ratio of 1:1 for combination therapy of the two APIs. The purified co-crystal was found to be more efficient compared to the compounds present individually. Further analysis of the physiochemical properties and molecular mechanisms of the isolated co-crystal in different cancer cells is warranted for its application in therapeutics.

Salam Asbin Singh

Asem Robinson Singh

Atom Rajiv Singh

Anoubam Sujita Devi

Minhaz Korimayum

Lisam Shanjukumar Singh

Discovery of a Novel Co-crystal of Chrysin and Oroxylin a with Anticancer Properties from Leaves of Oroxylum indicum

从木蝴蝶叶中发现具有抗癌特性的白杨素与黄芩素新型共晶

AXL, a receptor tyrosine kinase, has emerged as a critical player in tumorigenesis, metastasis, and resistance to conventional therapies. Its aberrant activation drives cell proliferation, survival, and angiogenesis, making it an attractive target for cancer treatment. In recent years, significant progress has been made in the development of AXL inhibitors. Chemical approaches have led to the discovery of small molecules that selectively bind to and inhibit AXL, disrupting its downstream signaling pathways. These inhibitors exhibit diverse structural features, including ATP-competitive and allosteric binding modes, offering potential advantages in terms of selectivity and potency. In addition to chemical approaches, biological strategies have also been explored to target AXL. These include the use of monoclonal antibodies, which can neutralize AXL ligands or induce receptor internalization and degradation. Furthermore, gene therapy techniques have been investigated to downregulate AXL expression or disrupt its signaling pathways. Despite these advancements, challenges remain in the development of AXL inhibitors. Selectivity is a critical concern, as AXL shares homology with other receptor tyrosine kinases. Drug resistance is another obstacle, as cancer cells can develop mechanisms to evade AXL inhibition. Furthermore, to address these challenges, combination therapies are being explored, such as combining AXL inhibitors with other targeted agents or conventional treatments. In conclusion, developing AXL inhibitors represents a promising avenue for improving cancer treatment outcomes. Continued research efforts are essential to overcome the existing challenges and translate these compounds into effective clinical therapies.

Kamal Shah

Krishan Gopal

Shivendra Kumar

Sunam Saha

Emerging AXL Inhibitors in Oncology: Chemical and Biological Advances in Targeted Cancer Therapy

肿瘤学中新兴的AXL抑制剂：靶向癌症治疗的化学和生物学进展

This study aimed to develop an effective model that identifies high-risk breast cancer (BRCA) patients and optimizes clinical treatments.

Yi Luo

Li Liu

Zeyu Hou

Daigang Xiong

Rui Chen

A Novel Effective Models for Identifying BRCA Patients and Optimizing Clinical Treatments

一种用于识别BRCA患者和优化临床治疗的新型有效模型

Abstract: Breast cancer frequently occurs in women. Among the several types of breast cancers, almost 50% of breast cancers are caused by one or more gene mutations of the PI3K/mTOR/AKT pathway. Capivasertib, the first AKT inhibitor, was authorized by the US FDA on November 16, 2023.. It is used for the treatment of adult patients with hormone receptor-positive, human epidermal growth factor receptor 2 negative metastatic breast cancer with at least one alteration on PIK3CA/AKT1/PTEN. In this short perspective, Capivasertib’s physicochemical properties, synthesis, mechanism of action, binding mode, pharmacokinetics, drug interaction studies, and treatment-emergent adverse events are discussed.

SURYA K DE

Capivasertib: First Approved AKT inhibitor for the Treatment of Patients with Breast Cancer

卡帕塞替尼：首个获批用于乳腺癌患者治疗的AKT抑制剂

Background: Phytochemicals have long remained an essential component of the traditional medicine system worldwide. Advancement of research in phytochemicals has led to the identification of novel constituents and metabolites from phytochemicals, performing various vital functions ranging from antimicrobial properties to anticarcinogenic roles. This plant is traditionally used by local people to manage inflammation. In this study, we aim to extract and chemically profile the essential oil from the leaves of Cleistocalyx operculatus (Roxb.) Merr. &amp; Perry and study of the anti-inflammatory and anti-proliferative role of essential oil. Methods: The hydro distillation method was used for the extraction of essential oil, and the GC-MS was applied for the chemical profiling. The percentage of cell viability was calculated using a crystal violet assay, colony formation assay was performed using Semiquantitative PCR, Propodium iodite staining was used for cell death assay, and Western blotting was used to determine antibodies and proteins. Schrodinger 2015 software was used for molecular docking. Results: Myrcene, a monoterpene, constitutes 56% of the oil and could be attributed to its anti-inflammatory potential. Treatment of LPS-challenged mouse macrophages RAW264.7 cells with essential oil resulted in a decline in the inflammatory markers, such as IL-1β, TNFα, iNOS, COX-2, and NFκB. Further, essential oil inhibited cancer PC-3, A431, A549, and MCF-7 cell lines at concentrations lower than normal PNT2 and HEK-293 cell lines. This decline in proliferative potential can be attributed to a decline in anti-apoptotic proteins, such as procaspase 3 and PARP, an increase in CKIs, such as p21, and a decline in the Akt signaling responsible for survival. Conclusion: The essential oil of the plant Cleistocalyx operculatus may be a potential lead for anti-inflammatory and anti-proliferative function.

Vivek Pandey

Sumnath Khanal

Nerina Shahi

Rupak Parajuli

Achyut Adhikari

Yuba Raj Pokharel

Anti-Inflammatory and Anti-proliferative Role of Essential Oil of Leaves of Cleistocalyx operculatus (Roxb.) Merr. &amp; Perry

闭鞘姜（Cleistocalyx operculatus）叶精油的抗炎和抗增殖作用

Abbreviation	ACAMC
Journal Impact	2.71
Quartiles(Global)	ONCOLOGY(Q3)

ISSN	1871-5206, 1875-5992
h-index	108

Publication Information	Publisher: Bentham Science Publishers，Publishing cycle: Monthly，Journal Type: journal，Open Access Journals: No
Basic data	Year of publication: 2006，Proportion of original research papers: 63.41%，Self Citation Rate:3.80%， Gold OA Rate: 1.69%
Average review cycle	网友分享经验：偏慢,4-8周
Average recruitment ratio	网友分享经验：较易

Anti-Cancer Agents in Medicinal Chemistry

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Current Expansions and Future Perspectives in Anticancer Drug Therapy.

Reactive Oxygen Species (ROS): Key Components in Cancer Therapies

Novel Arcyriaflavin-A Derivatives as PIM Kinase Inhibitors for Treating Cancer

Discovery of a Novel Co-crystal of Chrysin and Oroxylin a with Anticancer Properties from Leaves of Oroxylum indicum

Emerging AXL Inhibitors in Oncology: Chemical and Biological Advances in Targeted Cancer Therapy

A Novel Effective Models for Identifying BRCA Patients and Optimizing Clinical Treatments

Discovery of a Novel Co-crystal of Chrysin and Oroxylin a with Anticancer Properties from Leaves of Oroxylum indicum

Emerging AXL Inhibitors in Oncology: Chemical and Biological Advances in Targeted Cancer Therapy

Capivasertib: First Approved AKT inhibitor for the Treatment of Patients with Breast Cancer

Anti-Inflammatory and Anti-proliferative Role of Essential Oil of Leaves of Cleistocalyx operculatus (Roxb.) Merr. & Perry