Anti-cancer agents in medicinal chemistry
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Anticancer Agents Med Chem · Jan 2019
ReviewCan Combined Therapy Benefit Immune Checkpoint Blockade Response in Hepatocellular Carcinoma?
Hepatocellular Carcinoma (HCC) is one of the most common cancers with high mortality rate. The effects of most therapies are limited. The Immune Checkpoint Blockade (ICB) improves the prognosis in multiple malignancies. The application of immune checkpoint blockade to hepatocellular carcinoma patients has recently started. Early phase clinical trials have shown some benefits to cancer patients. ⋯ ICB is a promising therapy for advanced HCC patients. Combined therapy exhibits a great potential to enhance ICB response in these patients. The better understanding of the factors influencing the sensitivity of ICB and more clinical trials will consolidate the efficiency and minimize the adverse effects of ICB.
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In spite of major technological advances in conventional therapies, cancer continues to remain the leading cause of mortality worldwide. Phytochemicals are gradually emerging as a rich source of effective but safer agents against many life-threatening diseases. ⋯ Although numerous potent synthetic drugs have been introduced for cancer chemotherapy, yet their serious toxicity concerns to normal cells apart from drug resistance have emerged as the major obstacles for their clinical utility over a prolonged duration of time. Current status and potential of phytochemicals and their derivatives in cancer therapy have been briefly reviewed in the present manuscript.
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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.