scholarly journals Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1615 ◽  
Author(s):  
Jyothi Dhuguru ◽  
Rachid Skouta
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Basic Mechanism ◽  
Small Cell ◽  
Small Cell Lung ◽  
Dna Topoisomerase ◽  
Histone Deacetylase Inhibition ◽  
Lung Cancers ◽  
Drug Candidates

Lung cancer is the leading cause of death in men and women worldwide, affecting millions of people. Between the two types of lung cancers, non-small cell lung cancer (NSCLC) is more common than small cell lung cancer (SCLC). Besides surgery and radiotherapy, chemotherapy is the most important method of treatment for lung cancer. Indole scaffold is considered one of the most privileged scaffolds in heterocyclic chemistry. Indole may serve as an effective probe for the development of new drug candidates against challenging diseases, including lung cancer. In this review, we will focus on discussing the existing indole based pharmacophores in the clinical and pre-clinical stages of development against lung cancer, along with the synthesis of some of the selected anti-lung cancer drugs. Moreover, the basic mechanism of action underlying indole based anti-lung cancer treatment, such as protein kinase inhibition, histone deacetylase inhibition, DNA topoisomerase inhibition, and tubulin inhibition will also be discussed.

Exhaustive Review on Lung Cancers: Novel Technologies

2019 ◽  
Vol 15 (9) ◽  
pp. 873-883
Author(s):  
Sajad Khan ◽  
Shahid Ali ◽  
Muhammad
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Immune Therapy ◽  
Small Cell ◽  
X Rays ◽  
Small Cell Lung ◽  
Microscopic Appearance ◽  
Lung Cancers ◽  
Novel Technologies

Background:Lung cancers or (Bronchogenic-Carcinomas) are the disease in certain parts of the lungs in which irresistible multiplication of abnormal cells leads to the inception of a tumor. Lung cancers consisting of two substantial forms based on the microscopic appearance of tumor cells are: Non-Small-Cell-Lung-Cancer (NSCLC) (80 to 85%) and Small-Cell-Lung-Cancer (SCLC) (15 to 20%).Discussion:Lung cancers are existing luxuriantly across the globe and the most prominent cause of death in advanced countries (USA & UK). There are many causes of lung cancers in which the utmost imperative aspect is the cigarette smoking. During the early stage, there is no perspicuous sign/symptoms but later many symptoms emerge in the infected individual such as insomnia, headache, pain, loss of appetite, fatigue, coughing etc. Lung cancers can be diagnosed in many ways, such as history, physical examination, chest X-rays and biopsy. However, after the diagnosis and confirmation of lung carcinoma, various treatment approaches are existing for curing of cancer in different stages such as surgery, radiation therapy, chemotherapy, and immune therapy. Currently, novel techniques merged that revealed advancements in detection and curing of lung cancer in which mainly includes: microarray analysis, gene expression profiling.Conclusion:Consequently, the purpose of the current analysis is to specify and epitomize the novel literature pertaining to the development of cancerous cells in different parts of the lung, various preeminent approaches of prevention, efficient diagnostic procedure, and treatments along with novel technologies for inhibition of cancerous cell growth in advance stages.

scholarly journals Possible involvement of the Hedgehog and PDPK1–Akt pathways in the growth and migration of small-cell lung cancer

2021 ◽  
Vol 49 (5) ◽  
pp. 030006052110165
Author(s):  
Naiwang Tang ◽  
Bin Hu ◽  
Yin Zhang ◽  
Zhiwei Chen ◽  
Ronghuan Yu
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Molecular Mechanisms ◽  
Patient Characteristics ◽  
Small Cell ◽  
Small Cell Lung ◽  
Lung Cancers ◽  
And Migration ◽  
Proliferation And Migration

Background Small-cell lung cancer (SCLC) accounts for approximately 15% to 20% of all lung cancers, and it is the leading cause of tumor-related deaths globally. This study explored the molecular mechanisms underlying the development of SCLC. Methods The correlations of phosphoinositide-dependent kinase-1 (PDPK1), p-Akt, and Hedgehog expression with patient characteristics were analyzed using SCLC specimens, and their expression was measured in BEAS-2B cells (control) and the SCLC cell lines H82, H69, H446, H146, and H526. Transfection experiments were performed to inhibit or activate gene expression in cells. We then measured the proliferation and migration of H146 cells. Results PDPK1, p-Akt, and Hedgehog expression was significantly higher in SCLC tissues, and their expression was correlated with patient characteristics. p-Akt expression was significantly correlated with Hedgehog expression. In H146 cells, PDPK1 and p-Akt were significantly upregulated. Silencing of PDPK1 or Akt and inhibition of Hedgehog significantly inhibited the proliferation and migration of H146 cells. PDPK1 and Akt affected Hedgehog expression, but Hedgehog did not affect PDPK1 or p-Akt expression. Conclusions The interaction between the PDPK1–Akt pathway and the Hedgehog pathway influences the prognosis, growth, and migration of SCLC.

scholarly journals Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer

MedChemComm ◽  
2017 ◽  
Vol 8 (10) ◽  
pp. 1914-1918
Author(s):  
Lian-Xiang Luo ◽  
Ying Li ◽  
Yu-Zhen Niu ◽  
Yu-Wei Wang ◽  
Qian-Qian Wang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Fusion Protein ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Kinase Inhibitor ◽  
Small Cell ◽  
Small Cell Lung ◽  
Lung Cancers ◽  
Alk Inhibitor

Herein, we reported 5067-0952, a potent ALK inhibitor with pharmacological efficacy in non-small cell lung cancers harboring the ALK fusion oncogene.

scholarly journals Small cell lung cancer transformation during antitumor therapies: A systematic review

Open Medicine ◽  
2021 ◽  
Vol 16 (1) ◽  
pp. 1160-1167
Author(s):  
Xing Chai ◽  
Xinru Zhang ◽  
Wenqian Li ◽  
Jin Chai
Keyword(s):  
Lung Cancer ◽  
Drug Resistance ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Treatment Strategies ◽  
Small Cell ◽  
Small Cell Lung ◽  
Lung Cancers ◽  
Histological Transformation ◽  
Nsclc Patients

Abstract Lung cancer is the most common cause of cancer-related death. Non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) are the two major histological categories of lung cancers. Drug resistance is a great challenge for cancer treatment, and histological transformation from NSCLC to SCLC is one of the mechanisms underlying drug resistance in NSCLC patients. SCLC-transformed patients show combined characteristics of NSCLC and SCLC; however, they lack timely diagnoses and effective treatment strategies. Thus, we reviewed the clinical characteristics of SCLC transformation patients with a literature search to enhance clinical consciousness, diagnosis, and personalized treatment for patients with it.

scholarly journals Systemic Chemotherapy for Progression of Brain Metastases in Extensive-Stage Small Cell Lung Cancer

2015 ◽  
Vol 2015 ◽  
pp. 1-3 ◽  
Author(s):  
Nagla Abdel Karim ◽  
Ananta Bhatt ◽  
Lauren Chiec ◽  
Richard Curry
Keyword(s):  
Lung Cancer ◽  
Brain Metastases ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Systemic Chemotherapy ◽  
Case Series ◽  
Small Cell ◽  
Small Cell Lung ◽  
Lung Cancers ◽  
Lung Cancer Patients

Lung cancer is the most common cause of cancer related mortality in men and women. Approximately 15% of lung cancers are small cell type. Chemotherapy and radiation are the mainstay treatments. Currently, the standard chemotherapy regimen includes platinum/etoposide. For extensive small cell lung cancer, irinotecan and cisplatin have also been used. Patients with relapsed small cell lung cancer have a very poor prognosis, and the morbidity increases with brain metastases. Approximately 10%–14% of small cell lung cancer patients exhibit brain metastases at the time of diagnosis, which increases to 50%–80% as the disease progresses. Mean survival with brain metastases is reported to be less than six months, thus calling for improved regimens. Here we present a case series of patients treated with irinotecan for progressive brain metastases in small cell lung cancer, which serves as a reminder of the role of systemic chemotherapy in this setting.

scholarly journals Oncothermia with Chemotherapy in the Patients with Small-Cell Lung Cancer

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Doo Yun Lee ◽  
Seok Jin Haam ◽  
Tae Hoon Kim ◽  
Jae Yun Lim ◽  
Eun Jung Kim ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
Combined Therapy ◽  
Small Cell ◽  
Rank Test ◽  
Small Cell Lung ◽  
Lung Cancers ◽  
Long Survival ◽  
Survival Case

Small-cell lung cancer (SCLC) is one of the most aggressive and lethal forms of lung cancers. Chemotherapy and radiotherapy would be standard modality for SCLC with median survival being less than 4 months only. Complementary treatment to chemotherapy is desired. Oncothermia will be one of the candidates to this addition. We have made a study of 31 SCLC patients from April 2006 to March 2012. 23 cases were treated with combined chemotherapy and oncothermia, and 8 cases were treated with chemotherapy alone. Three patients from 14 patients (14/31) died in the study period; there were equal numbers in the two arms, including one long survival case of 28 months and one of 26 months, in the combination and chemo-group, respectively .16 patients (16/31) are alive: 4 patients with chemotherapy only, including one long survival case of 28.7 months, and 11 cases with combined therapy including three long survival cases of more than 3 years. We conclude that the combined use of chemotherapy and oncothermia has significantly enhanced the survival rate in comparison with the use of chemotherapy alone (log-rank test: P value < 0.02).

scholarly journals Significant Role of Nanoparticles as a Drug Delivery System for Cancer Treatment

2021 ◽  
pp. 383-423
Author(s):  
Alireza Heidari ◽  
Ricardo Gobato ◽  
Abhijit Mitra
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lung Cancer ◽  
The United States ◽  
Small Cell ◽  
Small Cell Lung ◽  
Lung Cancers ◽  
Dna Mutations ◽  
Phase 2 Clinical Trial ◽  
Keywords Cancer

According to the results of a global phase 2 clinical trial, the new drug sotorasib reduces tumor size and promises to improve and increase survival in patients with lung tumors caused by specific DNA mutations. It is designed to counteract the effects of mutations that are seen in about 13% of patients with non-small cell lung adenocarcinoma (a common type of lung cancer). The Food and Drug Administration (FDA) on May 28 approved the drug as a targeted treatment for patients with small cell lung cancer whose tumors express a specific mutation called G12C in the KRAS gene. Small cell lung cancer accounts for more than 80% of lung cancers. More than 200,000 new cases of non-small cell lung cancer are diagnosed in the United States each year. Keywords: Cancer; Cells; Tissues; Tumors; Prevention; Prognosis; Diagnosis; Imaging; Screening, Treatment; Management

scholarly journals Role of SOX Protein Groups F and H in Lung Cancer Progression

Cancers ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 3235
Author(s):  
Mateusz Olbromski ◽  
Marzenna Podhorska-Okołów ◽  
Piotr Dzięgiel
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cancer Progression ◽  
Cell Lung Cancer ◽  
Transcript Level ◽  
Small Cell ◽  
Gene Transcript ◽  
Small Cell Lung ◽  
Lung Cancers

The SOX family proteins are proved to play a crucial role in the development of the lymphatic ducts and the cardiovascular system. Moreover, an increased expression level of the SOX18 protein has been found in many malignances, such as melanoma, stomach, pancreatic breast and lung cancers. Another SOX family protein, the SOX30 transcription factor, is responsible for the development of male germ cells. Additionally, recent studies have shown its proapoptotic character in non-small cell lung cancer cells. Our preliminary studies showed a disparity in the amount of mRNA of the SOX18 gene relative to the amount of protein. This is why our attention has been focused on microRNA (miRNA) molecules, which could regulate the SOX18 gene transcript level. Recent data point to the fact that, in practically all types of cancer, hundreds of genes exhibit an abnormal methylation, covering around 5–10% of the thousands of CpG islands present in the promoter sequences, which in normal cells should not be methylated from the moment the embryo finishes its development. It has been demonstrated that in non-small-cell lung cancer (NSCLC) cases there is a large heterogeneity of the methylation process. The role of the SOX18 and SOX30 expression in non-small-cell lung cancers (NSCLCs) is not yet fully understood. However, if we take into account previous reports, these proteins may be important factors in the development and progression of these malignancies.

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