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Anti-cancer Agents in Medicinal Chemistry

Ebrahim Saeedian Moghadam, Maryam Hossein Poor Tehrani, René Csuk, Lucie Fischer, Mohammad Ali Faramarzi, Arezoo Rashidi, Iraj Javadi, Mohsen Amini
Considering the importance to find highly active anticancer agents, we investigated the synthesis and cytotoxic activity of twenty seven 2,4-disubstituted quinazoline derivatives. The cytotoxicity of compounds 1-27 was tested in SRB assays employing five different human tumor cell lines showing four compounds, 2, 9, 16 and 26, being highly cytotoxic with IC50 values ranging between 2.1 and 14.3 µM. The possible mode of action of compounds, 2, 9, 16 and 26, and the taxol binding site of the protein tubulin, an important goal for antimitotic drugs, was also studied by molecular docking followed by an investigation of the effects of compounds 9 and 16 on the polymerization of tubulin using a commercially available assay kit...
March 14, 2019: Anti-cancer Agents in Medicinal Chemistry
Arezoo Rahimian, Majid Mahdavi, Reza Rahbarghazi, Hojjatollah Nozad Charoudeh
OBJECTIVE: Many experiments have revealed the anti-tumor activity of spiro-quinazolinone derivatives on different cell types. Exposing KG1-a cells to N-(4- tert- butyl- 4'- oxo- 1'H- spiro [cyclohexane- 1, 2'- quinazoline]- 3'(4'H)- yl)- 4- methyl benzenesulfonamide (4t-CHQ), as an active sub-component of spiro-quinazolinone benzenesulfonamides, the experiment investigated the possible mechanisms that manifest the role of 4t-CHQ in leukemic KG1-a progenitor cells. Mechanistically, the inhibitory effects of 4t-CHQ on KG1-a cells emerges from its madulating function on expression of Bax/Bcl2 and suvinin proteins...
March 13, 2019: Anti-cancer Agents in Medicinal Chemistry
Shui-Ming Bao, Qing-Hui Hu, Wen-Ting Yang, Yao Wang, Yin-Ping Tong, Wen-Dai Bao
Lung cancer is one of the leading cause of cancer death worldwide, the most common histological type of lung cancer is non-small cell lung cancer (NSCLC), whose occurrence and development is closely related to the mutation and amplification of epidermal growth factor receptors (EGFR). Currently , a series of targeted drugs were developed on the inhibition of EGFR,such as epidermal growth factor receptor-tyrosine kinase inhibitor(EGFR-TKI) and monoclonal antibody (McAb). These drugs have been widely used in clinic practices...
March 13, 2019: Anti-cancer Agents in Medicinal Chemistry
Kamalpreet Kaur, Vikas Jaitak
BACKGROUND: Breast Cancer (BC) is the second most common cause of cancer related deaths in women. Due to severe side effects and multidrug resistance, current therapies like hormonal therapy, surgery, radiotherapy and chemotherapy become ineffective. Also, the existing drugs for BC treatment are associated with several drawbacks such as poor oral bioavailability, non-selectivity and poor pharmacodynamics properties. Therefore, there is an urgent need for the development of more effective and safer anti BC agents...
March 12, 2019: Anti-cancer Agents in Medicinal Chemistry
Selvaraj Jubie, Neetu Yadav
Conventional drug discovery is a time overwhelming and expensive expedition with super less clinical preference achievement proportion intended for breast cancer therapy. Even if numerous novel approaches to conformation of anti-cancer drugs have been introduced for breast cancer therapy, they have up till now to be implemented in clinical practice. This tempting strategy, facilitate remarkable chance to take entire benefit of existing drugs. Despite drug repurposing significantly decrease the investigational period and cost, it has got many objection and issues...
March 12, 2019: Anti-cancer Agents in Medicinal Chemistry
Alice Barros Câmara, Igor Augusto Brandãob
BACKGROUND: Vitamin D (VD) deficiency affects individuals of different ages in many countries. VD deficiency may be related to several diseases, including cancer. OBJECTIVE: This study aimed to review the relationship between VD deficiency and cancer. METHOD: We describe the proteins involved in cancer pathogenesis and how those proteins can be influenced by VD deficiency. We also investigated a relationship between cancer death rate and solar radiation...
March 12, 2019: Anti-cancer Agents in Medicinal Chemistry
Kuldip D Upadhyay, Anamik K Shah
BACKGROUND: Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents. OBJECTIVE: The present study is aimed to evaluate a new series of pyrano[3,2-c]quinoline scaffolds derived from fusion of bioactive quinolone pharmacophore with structurally diverse aryl substituted chromene for its cytotoxicity...
March 8, 2019: Anti-cancer Agents in Medicinal Chemistry
Ahmed A Mahmoud, Wael M El-Sayed
BACKGROUND: The increase in cancer rate and the development of resistant tumors require the continuous search for new anticancer agents. AIM: This study aimed to analyze and identify the chemical constituents of Anisosciadium lanatum, and to investigate the antiproliferative activity of the identified constituents against various human cell lines (HepG2, MCF7, HT29, A549, and PC3) along with the possible molecular mechanisms involved. METHODS: The structure of the isolated compounds was determined by spectroscopic techniques including HR-FABMS, GC-MS, IR, and 400 MHz 1D and 2D NMR analyses (1H, 13C NMR, DEPT, 1H-1H COSY, HMQC, HMBC and NOESY)...
March 7, 2019: Anti-cancer Agents in Medicinal Chemistry
Fanghua Qiu, Lifang Liu, Yu Lin, Zetian Yang, Feng Qiu
BACKGROUND: Esophageal squamous cell carcinoma (ESCC), the most prevalent histologic subtype of esophageal cancer, is an aggressive malignancy with poor prognosis and a high incidence in the East. Corilagin, an active component present in Phyllanthus niruri L., has been shown to suppress tumor growth in various cancers. However, the effects of corilagin on ESCC and the mechanisms for its tumor suppressive function remain unknown. METHODS: Cell proliferation was measured by Cell Counting Kit-8 assay and colony formation assays...
March 7, 2019: Anti-cancer Agents in Medicinal Chemistry
Yu-Lian Xu, Xiao-Ming Jiang, Le-Le Zhang, Xiuping Chen, Zhang-Jian Huang, Jin-Jian Lu
BACKGROUND: Pemetrexed (PMT) is a multitargeted antifolate agent that is used for treating patients with non-small cell lung cancer (NSCLC). However, patients have presented clinical responses of drug resistance to PMT. OBJECTIVE: This study aimed to explore the underlying mechanisms of PMT resistance in NSCLC cells. METHODS: PMT-resistant NCI-H460/PMT cells were established by treating with PMT in a dosage-escalation manner. MTT assay and colony formation were performed to detect the cell proliferation...
March 7, 2019: Anti-cancer Agents in Medicinal Chemistry
Pritam N Dube, Nikhil S Sakle, Sachin A Dhawale, Shweta A More, Santosh N Mokale
A series of novel 6-methyl-3-(3-oxo-1-phenyl-3-(4-(2-(piperidin-1-yl)ethoxy)phenyl)propyl)-2H-chromen-2-one was designed, synthesized and screened for their Anti-Breast Cancer activity against estrogen receptor-positive MCF-7, ZR-75-1 and negative MDA-MB-435 human breast cancer cell lines. Among the synthesized compounds C-3, C-5 and C-15 were showing potent cytotoxicity against estrogen receptor-positive MCF-7. The potent cytotoxic compounds C-3, C-5 and C-15 were further evaluated for in vivo anti-cancer activity by MNU (N-methyl-N-nitrosourea) induced mammary carcinoma in female Sprague-Dawley rats...
March 7, 2019: Anti-cancer Agents in Medicinal Chemistry
Marin Neykov Marinov, Emilia Dimitrova Naydenova, Georgi Tsvetanov Momekov, Rumyana Yordanova Prodanova, Nadezhda Vasileva Markova, Yulian Tenchev Voynikov, Neyko Marinov Stoyanov
BACKGROUND: The 1,8-Naphthalimides constitute an important class of biologically active, DNA-binding compounds. There are no available data on the synthesis of 1,8-naphthalimide derivatives with non-protein amino acids and their biological activity. The aims of this paper are to synthesis, structural characterization and cytotoxic activity of new 1-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)cycloalkane-1-carboxylic acids with 5-, 6-, 7-, 8- and 12-membered rings as well as 2-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)adamantane-2-carboxylic acid and 1-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid...
March 6, 2019: Anti-cancer Agents in Medicinal Chemistry
Magda F Mohamed, Hamdi M Hassaneen, Emad M Elzayat, Salwa M El-Hallouty, May El-Manawaty, Fatma M Saleh, Yasmin Mohamed, Dina El-Zohiry, Ghada Fahmy, Nesma Abdelaal, Nouran Hassanin, Nouran Hossam
BACKGROUND: The hydrazonoyl halides are presently an important target in the field of medicinal chemistry. The interest in the chemistry of hydrazonoyl halides is a consequence of the fact that they undergo a wide variety of reactions which provide routes to a myriad of both heterocyclic and acyclic compounds. In addition, they have diverse biological activities such as antiviral, anthelmintic, antiarthropodal,, fungicidal, herbicidal, insecticidal, pesticidal, acaricidal and miticidal Activity correlated to the presence of hydrazonoyl halides...
March 6, 2019: Anti-cancer Agents in Medicinal Chemistry
Ghansham S More, Asha B Thomas, Sohan S Chitlange, Rabindra K Nanda, Rahul L Gajbhiye
Background& Objective: Nitrogen mustard derivatives form one of the major class of the anti-cancer agents according to the USFDA approved drugs. These are polyfunctional alkylating agents which are distinguished by a unique mechanism of adduct formation with the DNA that involves a cross-linking between guanine N-7 of one strand of DNA with the other. The generated cross-linking is irreversible and leads to cell apoptosis. Thus, there is an upsurge in the interest to explore this class of anticancer alkylating agents...
March 5, 2019: Anti-cancer Agents in Medicinal Chemistry
HuiYu Li, Fei Luo, XiaoYu Li, XiFeng Fu, JieFeng He, YanZhang Tian, JunJun Zhu, XinYi Chu, HaoLiang Zhao
BACKGROUND: Multi Drug Resistance (MDR) is the phenomenon that cancers develop resistance to majority of chemotherapy drugs and is a serious obstacle to the treatment for hepatocellular carcinoma (HCC). Polo-Like Kinase 1 (PLK1) is a serine/threonine kinase associated with tumor growth and clinical prognosis in HCC and BI2536 is its potent inhibitor with IC50 of 0.83 nM. AIMS: To test whether the down-regulation of PLK1 by its inhibitor BI2536 would have beneficial effects on the reversal of MDR in HCC cells...
March 1, 2019: Anti-cancer Agents in Medicinal Chemistry
Appavoo Umamaheswari, Ayarivan Puratchikody, Natarajan Hari
In recent times, we have reported the design and in silico studies of 52 hydroxamic acid derivatives bearing multi-substituent heteroaromatic rings with chiral amine linker as isoform selective histone deacetylase 8 inhibitors (HDAC8i). Wherein, the report suggested that the presence of chiral amine is a prerequisite to occupy the second binding site of HDAC8. Based on these preliminary results, five compounds were shortlisted and synthesized by microwave assisted approach and high yielding synthetic protocol...
March 1, 2019: Anti-cancer Agents in Medicinal Chemistry
Lijuan Wang, Ziqian Zhang, Rui Ge, Jian Zhang, Wenli Liu, Kuanhou Mou, Shemin Lv, Xin Mu
Skin photoaging, skin inflammation and skin cancer are related with excessive exposure to solar ultraviolet light (solar-UV). PDZ-binding kinase/T-LAK cell-originated protein kinase (PBK/TOPK), a member of the serine/threonine protein kinase, which regulates the signaling cascades of p38 mitogen-activated protein kinase (p38 MAPK) and extracellular signal regulated kinase 1/2 (ERK1/2). PBK/TOPK plays a significant role in solar-UV-induced cutaneous basal cell carcinoma (cutaneous-BCC), and targeting PBK/TOPK can be supposed to treat and prevent cutaneous-BCC...
March 1, 2019: Anti-cancer Agents in Medicinal Chemistry
Habib Zarredar, Safar Farajnia, Khalil Ansarin, Behzad Baradaran, Maryam Aria, Milad Asadi
BACKGROUND: Lung cancer is the leading cause of cancer-related death with less than 5-year survival rate for both men and women worldwide. EGFR and MAPK signaling pathways have a critical role in proliferation and progression of various cancers, including lung cancer. P38 map kinase plays the different role in various tissue hence show a tissue-dependent behavior. It acts as an oncogene in some tissues while plays as tumor suppressor in other some tissues. The aim of this study was to investigate the combined effect of P38 αspecific siRNA and EGFR inhibitor on apoptosis and proliferation of A549 lung cancer cell line...
March 1, 2019: Anti-cancer Agents in Medicinal Chemistry
Kirubel Teshome Tadele, Tilahun Wubalem Tsega
BACKGROUND: Schiff bases and their metal complexes are emerging as key classes of medicinal compounds, possessing an enormous potential of biological activities like anticancer, anticonvulsant and antioxidant etc. The aim of this review is to examine the anticancer activity of different classes of Schiff bases and their metal complexes. METHODS: Anticancer activity of the already synthesized as well as the novel Schiff bases and their metal complexes was studied using different assays such as 3- [4,5-dimethyltiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT), PI staining, Sulforhodamine, Allium cepa, Sulfo- Rhodamine-B-stain(SRB), viability and potato disc against various human and animal cancer cell lines...
February 27, 2019: Anti-cancer Agents in Medicinal Chemistry
İlkay Küçükgüzel, Bahadır Bülbül
BACKGROUND: Cancer is one of the top killing disease worldwide. Since inflammation is considered to be one of the known characteristics of cancer, the activity of PGE2 has been paired with different tumorigenetic steps such as increased tumor cell proliferation, resistance to apoptosis, increased invasiveness, angiogenesis and immunosuppression. OBJECTIVE: It has been succesfully demonstrated that inhibition of mPGES-1 prevented inflammation in preclinical studies...
February 27, 2019: Anti-cancer Agents in Medicinal Chemistry
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