Anti-cancer agents in medicinal chemistry
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Anticancer Agents Med Chem · Jan 2018
ReviewEnasidenib: First Mutant IDH2 Inhibitor for the Treatment of Refractory and Relapsed Acute Myeloid Leukemia.
Acute myeloid leukemia is the collective name for different types of leukemias of myeloid origin affecting blood and bone marrow. The overproduction of immature myeloblasts (white blood cells) is the characteristic feature of AML, thus flooding the bone marrow and reducing its capacity to produce normal blood cells. USFDA on August 1, 2017, approved a drug named Enasidenib formerly known as AG-221 which is being marketed under the name Idhifa to treat R/R AML with IDH2 mutation. The present review depicts the broad profile of enasidenib including various aspects of chemistry, preclinical, clinical studies, pharmacokinetics, mode of action and toxicity studies. ⋯ Enasidenib or AG-221was introduced by FDA as an anticancer agent which was developed as a first in class, a selective allosteric inhibitor of the tumor target i.e. IDH2 for Relapsed or Refractory AML. Phase 1/2 clinical trial of Enasidenib resulted in the overall survival rate of 40.3% with CR of 19.3%. Phase III trial on the Enasidenib is still under process along with another trial to test its potency against other cell lines. Edasidenib is associated with certain adverse effects, which can be reduced by investigators by designing its newer derivatives on the basis of SAR studies. Hence, it may come in the light as a potent lead entity for anticancer treatment in the coming years.
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Anticancer Agents Med Chem · Jan 2018
ReviewAmygdalin from Apricot Kernels Induces Apoptosis and Causes Cell Cycle Arrest in Cancer Cells: An Updated Review.
Amygdalin is a cyanogenic glycoside which is described as a naturally occurring anticancer agent. Current review highlights apoptosis-inducing attributes of amygdalin towards different cancers and its potential application as an anti-cancer agent in cancer therapy. ⋯ The current review epitomizes published information and provides complete interpretations about all known anti-cancer mechanisms of amygdalin, possible role of naturally occurring amygdalin in fight against cancer and mistaken belief about cyanide toxicity causing potential of amygdalin. However, well-planned clinical trials are still needed to be conducted to prove effectiveness of this substance in vivo and to get approval for human use.
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Anticancer Agents Med Chem · Jan 2018
ReviewCritical microRNAs in Lung Cancer: Recent Advances and Potential Applications.
MicroRNAs (miRNAs) play an important role in the regulation of various genes involved in cell growth, development and the maintenance of body homeostasis. They are closely linked to different human diseases, particularly in cancers. Amplification and overexpression of some miRNAs that are called 'oncomiRs' or down-regulation of tumor suppressor miRNAs are associated with genetic alterations that are sufficient to drive tumorigenesis in humans. Lung cancer is the leading cause of cancer-related deaths worldwide. The high mortality rate of lung cancer is not changed even with recent advances in cancer treatment. Several studies demonstrated that miRNAs are involved in the pathogenesis of lung cancer that they negatively or positively regulate gene and protein expression by acting as oncogenes or tumor suppressors. ⋯ Many research studies have shown that a combination of chemotherapy plus knockdown or mimicking microRNA is effective and useful in the cancers treatment like lung cancer.
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Anticancer Agents Med Chem · Jan 2018
Oxaliplatin Regulates Chemotherapy Induced Peripheral Neuropathic Pain in the Dorsal Horn and Dorsal Root Ganglion via the Calcineurin/NFAT Pathway.
The aim of this study was to investigate the mechanism of oxaliplatin in the induction of neuropathic pain as a symptom of Chemotherapy-Induced Peripheral Neuropathy (CIPN). ⋯ It was the first time to prove that oxaliplatin-induced neuropathic pain was correlated to the activation of the CaN/NFAT pathway in our rat model. This finding can provide a new direction to explore the mechanism of oxaliplatin-induced neuropathic pain.
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Anticancer Agents Med Chem · Jan 2018
Biomarkers in Non-Small Cell Lung Cancer: Perspectives of Individualized Targeted Therapy.
The understanding of cancer has evolved into a complex disease, which has heterogeneous characteristics between different patients, and more than that, a broad range of genetically distinct cells in the same tumor. Chronic and non-transmissible diseases such as cancer have become even more important worldwide and advances in their characterization and properties are running out. In a suitable setting, early diagnosis of cancer and proper treatment are essential to overcome the barriers of tumor healing and quality assurance of the patient's life. The studies included in the analysis were independently retrieved by the authors. The text words included "Non-Small Cell Lung Cancer," "NSCLC," "biomarkers in NSCLC" and "gene in NSCLC"." We were used to perform a systematic literature search in the PubMed and Web of Science databases. There was limit on the start date for published articles (2001), and the search ended in December 2017. For a more comprehensive analysis, articles were only in English. ⋯ This review highlights the importance of molecular diagnosis of mutations in lung cancer, driving to individualized therapy with the intent of getting a better response to treatment and improving patients' quality of life.