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Anti-cancer Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28443517/1-3-4-oxadiazoles-as-telomerase-inhibitor-potential-anticancer-agents
#1
Shalini Bajaj, Partha Pratim Roy, Jagadish Singh
Cancer is a rapidly growing disease of current era which poses a major life threaten situation to human beings. Continuous research is going on in the direction to develop effective molecules for the treatment of the cancer. These efforts include searching of more active heterocyclic compounds possessing potential anti-cancer activity. The 1,3,4-Oxadiazole scaffold is a five member heterocyclic ring having versatile activities and created interest for synthetic organic and medicinal chemists for the designing of novel compounds having anti-cancer activity...
April 24, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443516/synergistic-effect-of-graphene-oxide-coated-nanotised-apigenin-with-paclitaxel-go-na-ptx-a-ros-dependent-mitochondrial-mediated-apoptosis-in-ovarian-cancer
#2
Manish Kumar Pal, Shyam Pyari Jaiswar, Ashish Dwivedi, Shruti Goyal, Vinay Nand Dwivedi, Anumesh Kumar Pathak, Vinod Kumar, Pushp Lata Sankhwar, Ratan Singh Ray
Ovarian cancer is most lethal among all gynecologic malignancies. Paclitaxel (PTX) is well used chemotherapeutic regimen for cancer control; however its undesired toxicity has been always a matter of concern for clinicians. Here we used the graphene oxide coated nanotised apigenin (GO-NA) as chemo sensitizing agent to enhance the efficacy of paclitaxel to overcome the limitations of chemotherapy. GO and GO-Apigenin was prepared by modified Hummers method and the nanoparticles were characterized by dynamic light scattering and transmission electron microscopy Human ovarian adenocarcinomas (SKOV-3) cells was treated by DMSO, Group I (Control)-McCoy's 5A Medium, Group II-Paclitaxel (5nM) alone, Group III- Nanotised Apigenin (GO-NA-10μM) Group IV- Paclitaxel (5nM) + GO-NA (10μM)...
April 24, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425859/synthesis-characterization-and-inducing-tumor-cell-apoptosis-of-two-ru-ii-complexes-containing-guanidinium-as-ligands
#3
Jing Sun, Wen-Xiu Chen, Xing-Dong Song, Shu-Fen He, Jia-Xi Chen, Jun Mei, Xiao-Xian Zhu, Tie Wu
Two new ruthenium(II) complexes containing guanidinium as ligands, [Ru(dip)2(L1)]3+ (Ru1) and [Ru(dip)2(L2)]3+ (Ru2) (dip = 4,7-diphenyl-1,10-phenanthroline; L1 = 1-(4-(1H-imidazo[4,5-f][1,10]phenanthrolin-2-yl)phenyl)guanidine cation; L2 = 1-(3-(1H-imidazo[4,5-f][1,10]phenanthrolin-2-yl)phenyl)guanidine cation) have been synthesized and characterized. Both complexes display higher cytotoxicity against several cancer cell lines compared to cisplatin and are less cytotoxic on the nontumorigenic cell line LO2...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425858/nano-encapsulation-of-dietary-phytoconstituent-capsaicin-on-emulsome-evaluation-of-anticancer-activity-through-the-measurement-of-liver-oxidative-stress-in-rats
#4
Tapan Kumar Giri, Kaustav Pramanik, Tapan Kumar Barman, Subhasis Maity
Protective effects of capsaicin (CAP) loaded nano-emulsomes (EML) was evaluated against the oxidative stress of rat livers induced through sodium fluoride (NaF). EML was prepared by thin film hydration method that is development of thin lipid film followed by hydration and sonication. EML was characterized by Fourier transform infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) techniques. In vitro drug release study of optimized formulation showed that 50% of CAP was released within 50.21 min while 85% CAP was released in 227...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425857/antioxidant-properties-of-fractions-for-unripe-fruits-of-capsicum-annuum-l-var-conoides
#5
Chung-Yi Chen, Ching-Yu Yen, Gao-Mai Shen, Tzu-Jung Yu, Yi-Shin Liao, Ru-In Jian, Sheng-Chieh Wang, Jen-Yang Tang, H-W Chang
BACKGROUND: Capsicum plant, especially for C. annuum, is an abundant resource for bioactive antioxidants, but few studies have examined the unripe fruit part of the Capsicum plant. OBJECTIVE: MeOH extract of unripe fruits of C. annuum L. var. conoides (UFCA) was chromatographed over a silica gel column using a gradient of CH2Cl2/MeOH as eluent to produce 9 fractions. Antioxidant activities are evaluated along with cell viabilities of 9 fractions of UFCA. METHOD: The antioxidant properties were analyzed in terms of total phenol content (TPC), total flavonoid content (TFC), 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2-azinobis (3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) radical scavenging, ferric reducing, and ferrous ion-chelating ability...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425856/apicidin-inhibited-proliferation-and-invasion-and-induced-apoptosis-via-mitochondrial-pathway-in-non-small-cell-lung-cancer-glc-82-cells
#6
Jianye Zhang, Zhenzhu Lai, Wenjing Huang, Huiping Ling, Minting Lin, Sili Tang, Yun Liu, Yiwen Tao
Apicidin, an inhibitor of histone deacetylase obtained from the mangrove endophytic fungi Fusarium sp., showed a wide range of antiproliferative activity against various cancer cell lines. Apicidin has also been reported to induce apotosis via Fas/Fas ligand. Yet few studies have focused on mitochondrial pathway for its anti-tumor activity. Here, we evaluated its involved mitochondrial mechanism against lung cancer GLC-82 cells. Its structure was elucidated by MS and NMR spectroscopic data, and comparison of those data with published data...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425855/tumor-targeting-peptides-ligands-for-molecular-imaging-and-therapy
#7
Ning Zhao, Yeshan Qin, Hongguang Liu, Z Cheng
The aberrant proliferation of tumor cells and abundant vasculature in tumor tissues are closely correlated with receptors that are specifically dysregulated in tumor cells. These tumor-associated targets are critical in early diagnosis and therapy selection. Ligands such as antibodies, proteins, polypeptides and polysaccharides that specifically bind to these targets can significantly improve the detection and cure rate when used as tumor imaging probes or anti-tumor agents. Compared to other targeting ligands, peptides have attracted increasingly more attention in tumor diagnostics and therapeutics because of their small sizes, high affinity, stability, ease of modification and low immunogenicity...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425854/rationale-design-synthesis-cytotoxicity-evaluation-and-molecular-docking-studies-of-1-3-4-oxadiazole-analogues
#8
Mohamed Jawed Ahsan, Arun Choupra, Rakesh Kumar Sharma, Surender Singh Jadav, Mohd Zaheen Hassan, Mohammed Afroz Bakht, Pannala Padmaja, Abdulmalik Bin Saleh Al-Tamimi, Mohammed H Geesi
We report herein, the synthesis of two new series of oxadiazole analogues, and their cytotoxicity evaluation. The oxadiazole analogues (5a-h and 12a-h) were structurally related to the heterocyclic (1,3,4- oxadiazole) linked aryl core of IMC-038525 (tubulin polymerization inhibitor), NSC 776715, and NSC 776716, with further modification by incorporating methylene linker. The title compounds (5a-h and 12a-h) were synthesized in good yields, and were characterized by IR, NMR, and mass spectral data. The cytotoxicity evaluation was carried out according to the National Cancer Institute (NCI US) Protocol against NCI-60 human cell lines derived from nine different panels...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425853/evaluation-of-the-in-vitro-chemosensitivity-and-correlation-with-clinical-outcomes-in-lung-cancer-using-the-atp-tca
#9
Zhiyao Chen, Shichao Zhang, Sheng Ma, Chang Li, Chun Xu, Yinfang Shen, Jun Zhao, Liyan Miao
BACKGROUND AND OBJECTIVE: Multiple drug resistance (MDR) to chemotherapeutic agents often leads to a failure to respond to chemotherapy. We utilized an in vitro chemosensitivity test to identify sensitive and effective chemotherapeutic drugs and further elucidated the correlation between the in vivo chemosensitivity and clinical outcomes. METHODS: Here, we evaluated the in vitro chemosensitivity and MDR of 120 lung cancer patients to eight single-drug chemotherapies and of 291 lung cancer patients to seven chemotherapy regimens using an ATP-based tumour chemosensitivity assay (ATP-TCA)...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425852/discovery-of-novel-2-amino-5-substituted-1-3-4-thiadiazole-derivatives-new-utilities-for-colon-cancer-treatment
#10
Vinit Raj, Amit Rai, Ashok K Singh, Amit K Keshari, Prakruti Harshvardhanbhai Trivedi, Balaram Ghosh, Umesh Kumar, Dinesh Kumar, Sudipta Saha
In this study, we designed and synthesized (VR1 to VR35) a novel series of 1,3,4-thiadiazole derivatives from 2-amino-5-(substituted)-1,3,4-thiadiazole condensed with substituted aldehyde or ketone in the presence of glacial acetic acid via Wolff-Kishner reduction. Further, synthesized compounds were characterized by FTIR, NMR (1H and 13C), MS and elemental analyses. Before the synthesis, docking studies were performed using various molecular targets of colon cancer like IL-2, IL-6, COX-2, caspase-3, and caspase-8...
April 19, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403785/apoptotic-effects-of-some-tetrahydronaphthalene-derivatives-on-k562-human-chronic-myelogenous-leukemia-cell-line
#11
Aslı Koç, Tulin Ozkan, Arzu Zeynep Karabay, Yalda Hekmatshoar, Ayse Selen Gurkan-Alp, Fugen Aktan, Zeliha Buyukbingol, Asuman Sunguroglu, Erdem Buyukbingol
BACKGROUND: Retinoids are synthetic and naturally occurring derivatives of vitamin A (retinol) which have been suggested to mediate inhibition of cancer cell growth and apoptosis. It has been reported that all trans retinoic acid (ATRA) exhibited suppressive effects on different types of leukemia including chronic myelogenous leukemia. OBJECTIVE: In the present study, we aim to find out the effects of 6 synthetic N-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalene-2-yl)-carboxamide derivatives (compound 6-12) on cell viability and apoptotic pathways in K562 human chronic myelogenous leukemia cell line...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403784/synthesis-characterization-of-4-anilino-6-7-dimethoxy-quinazoline-derivatives-as-potential-anti-angiogenic-agents
#12
Saligrama Devegowda Preethi, Balaji Kyathegowdanadoddi Srinivas, Prasanna Doddakunche Shivaramu, Swaroop Toreshettahally Ramesh, Shankar Jayarama, Rangappa KanchKanchugarakoppal Subbegowda, Lokesh Siddalingaiah Gowda
A series of novel 4-anilino-6,7-dimethoxy quinazoline derivatives were synthesized and characterized using 1H, 13C NMR and FT-IR and mass spectroscopic techniques. Cytotoxicity assays were performed for all compounds against different cell lines such as human colon carcinoma (HCT116), human chronic myeloid leukemia (K562) and human breast cancer (SKBR3) cell lines using 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide (MTT), Tryphan blue and Lactose dehydrogenase release assay. Among all compounds, RB4, RB7 showed moderate activity whereas RB1 showed most potent activity comparable with that of the standard drug cisplatin against all three cells lines...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403783/synthesis-and-evaluation-of-2-naphthaleno-trans-stilbenes-and-cyanostilbenes-as-anticancer-agents
#13
Nikhil R Madadi, Narsimha R Penthala, Amit Ketkar, Robert L Eoff, Vicenta Trujullo-Alonso, Monica L Guzman, Peter A Crooks
A series of novel 2-naphthaleno stilbenes (3a-3h) and cyanostilbenes (5a-5h) have been synthesized as analogs of resveratrol and DMU-212, and evaluated for their anticancer activity against a panel of 54 human cancer cell lines. The analog 5c ((Z)-3-(naphthalen-2-yl)-2-(3,4,5-trimethoxyphenyl) acrylonitrile) was significantly effective against four particular cancer cell lines: i.e. colon cancer cell line COLO 205, CNS cancer cell line SF 539 and melanoma cancer cell lines SK-MEL 5 and MDA-MB-435 with GI50 values of 22 nM, 25 nM, 23 nM and 21 nM, respectively...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403782/synthesis-cytotoxicity-and-antimicrobial-activity-of-new-enmein-type-kauranoid-diterpenoid-derivatives
#14
Dahong Li, Tong Han, Xu Hu, Kangtao Tian, Shengtao Xu, Tingting Zhou, Keguang Cheng, Zhanlin Li, Huiming Hua, Jinyi Xu
Eleven new enmein-type diterpenoid derivatives with different substituents and drug-like properties were designed and synthesized. The antimicrobial activities against E. coli, S. aureus, B. subtilis and M. albicans were disclosed. The results revealed that enmein-type diterpenoids showed more promising activities against tested gram-positive bacteria than gram-negative bacterium and fungus. Compound 9 with R of 2-quinolyl group exhibited the strongest antimicrobial activities with MIC values of 7.81 μg/ml and 0...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403781/design-synthesis-and-biological-evaluation-of-novel-1-3-thiazolidine-2-4-diones-as-anti-prostate-cancer-agents
#15
Ramakrishnan Elancheran, Kuppusamy Saravanan, Selvaraj Divakar, Sima Kumari, V Lenin Maruthanila, Senthamarikannan Kabilan, Muthaiah Ramanathan, Rajlakshmi Devi, Jibon Kotoky
Androgen receptor (AR) is an attractive target for the treatment of prostate cancer. Structural modification and molecular docking-based virtual screening approaches were imposed to identify the novel 1,3-thiazolidine-2,4-diones (TZDs) by using Schrödinger (Maestro 9.5). The best fit molecules (3-12 & 23-31) were synthesized and characterized using spectroscopic techniques, then in vitro antioxidant and anti-prostate cancer activities were evaluated. Further, the structure of the intermediate (18) was confirmed by single crystal XRD analysis...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403780/synthesis-of-novel-benzothiazole-piperazine-derivatives-and-their-biological-evaluation-as-acetylcholinesterase-inhibitors-and-cytotoxic-agents
#16
Enise Ece Gurdal, Bengisu Turgutalp, Hayrettin Ozan Gulcan, Tugba Erçetin, Mustafa Fethi Sahin, Irem Durmaz, Rengul Cetin Atalay, Quoc Dat Nguyen, Wolfgang Sippl, Mine Yarim
A new series of benzothiazole-piperazine derivatives were synthesized and a complete chemical characterization of the novel compounds was provided. In vitro cytotoxic activities were screened against colorectal (HCT-116), breast (MCF-7) and hepatocellular (Huh7) cancer cell lines by Sulforhodamine B assay. All compounds showed cytotoxic activity against hepatocellular (Huh7) and breast (MCF-7) cancer cell lines. Dihalo substituted benzylpiperazine derivatives (2a, 2e) had the highest cytotoxic activities in all tested cell lines...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403779/design-synthesis-and-biological-evaluation-of-betulinic-acid-derivatives-as-new-antitumor-agents-for-leukemia
#17
Fernanda Waechter, Gloria Santos Silva, Julia Willig, Cristiane Bernardes de Oliveira, Bruna Domingues Vieira, Daniela Barreto Trivella, Aline Rigon Zimmer, Andréia Buffon, Diogo André Pilger, Simone Gnoatto
Chronic myeloid leukemia (CML) is currently treated with imatinib, a Bcr-Abl inhibitor. However, resistance to this drug usually develops over time. Triptolide, a diterpenoid triepoxide, has been shown active against CML cells resistant to imatinib, acting mainly on the level of Bcr-Abl transcription inhibition. Here, we used the triterpene betulinic acid, a known proteasome inhibitor with potential antileukemic activity, as a scaffold for the generation of analogues with predicted triptolide biological activity...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403778/myc-decoy-oligodeoxynucleotide-inhibits-growth-and-modulates-differentiation-of-mouse-embryonic-stem-cells-as-a-model-of-cancer-stem-cells
#18
Behrooz Johari, Mina Ebrahimi-Rad, Faezeh Maghsood, Majid Lotfinia, Zohreh Saltanatpouri, Ladan Teimoori-Toolabi, Zahra Sharifzadeh, Morteza Karimipoor, Mehdi Kadivar
Myc (c-Myc) alone activates the embryonic stem cell-like transcriptional module in both normal and transformed cells. Its dysregulation might lead to increased cancer stem cells (CSCs) population in some tumor cells. Because of the technical limitations, difficulties of keeping CSCs in culture and their similarities with mouse embryonic stem cells (mESCs), we used the latter as a model cell of study to analyze the potential of differentiation therapy mediated by Myc decoy approach. To our best of knowledge this is the first report outlining the application of Myc decoy in transcription factor decoy "TFD" strategy for inducing differentiation in mESCs...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403777/potential-molecular-targets-of-ampelopsin-in-prevention-and-treatment-of-cancers
#19
Xianjuan Kou, Jingjing Fan, Ning Chen
Cancers have increasing threat to human health due to the limited treatment efficacy of chemotherapy and radiotherapy with a series of toxicity and side effects; therefore, the development and utilization of natural products with potential preventive and therapeutic efficacy, and less toxicity and side effects will be beneficial to promote the health of cancer patients. In this article, the activity of ampelopsin as a natural flavonoid and its underlying molecular mechanisms for the prevention and treatments of hepatic carcinoma, breast cancer, prostate cancer and melanoma through inhibiting cell proliferation, accelerating apoptosis, inducing reactive oxygen species (ROS) generation and endoplasmic reticulum (ER) stress, suppressing angiogenesis, invasion and metastasis, and synergizing the efficacy of other anti-cancer drugs have been summarized...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403776/eco-friendly-synthesis-of-pyrido-2-3-d-pyrimidine-analogs-and-their-anticancer-and-tyrosine-kinase-inhibition-activities
#20
Wael M El-Sayed, Abeer El-Naggar, Ali Khalil, Hala Zeidan
BACKGROUND: One of the promising scaffolds in drug discovery is the fused pyrimidine derivatives. OBJECTIVE AND METHOD: Efficient synthesis of a novel series of 18 new 1,8-naphthyridine-3-carbonitrile, 2-amino pyrido[2,3-d]pyrimidine derivatives via multi-component reactions of aromatic aldehydes, active methylene, and an aromatic amine under microwave irradiation and evaluation of their anticancer activity and possible mechanisms. RESULTS: Only compounds 5 (a-c) had a significant antiproliferative activity in hepatic HepG2 cells at submicromolar concentration (7...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
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