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Anti-cancer Agents in Medicinal Chemistry

Anna Pratima G Nikalje, Pramod Gawhane, Shailee Tiwari, Jaiprakash Sangshetti, Manoj Damale
In this work, a new series of diethyl ((1H-indole-3-yl)((5-phenyl-1,3,4-thiadiazole-2- yl)amino)methyl)phosphonate derivatives 6(a-j) were designed and synthesized in Ultrasound by green protocol using Kabachnik-Fields reaction. The structures of the synthesized compounds were confirmed by spectral analysis such as elemental analyses, IR, 1H NMR, 13C NMR, 31P NMR and mass spectra. The synthesized compounds 6(a-j) were appraised for their in vitro anticancer activity against human cancer cell lines such as SK-MEL-2 (melanoma), IMR-32 (Neuroblastoma), HT-29(Colon) and also on normal murine embryonic fibroblast NIH/3T3 by Sulforhodamine B (SRB) assay, using Adriamycin as a standard drug...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
Diana Wesselinova, Emilia D Naydenova, S Staykova, I G Goshev, L Vezenkov
BACKGROUND: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. OBJECTIVES: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). METHODS: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (human colorectal cancer cell line), MDA-MB-23 (human breast cancer cell line), Hep G-2 (human hepatocellular carcinoma cell line) and HeLa (cervical cancer cell line)...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
Khaled El-Adl, Abdel-Ghany A El-Helby, Rezk R A Ayyad, Helmy Sakr, Mamdouh M Ali, Fathalla Khedr
In view of their expected anticancer activity, novel triazolo[3,4-a]phthalazine derivatives 5-6a-o and 3-substituted-bis([1,2,4]triazolo)[3,4-a:4',3'-c]phthalazines 9a-b were designed, synthesized and evaluated for their anti-proliferative activity against two human tumor cell lines HCT-116 human colon adenocarcinoma and MCF-7 breast cancer. It was found that, compound 6o the most potent derivative against both HCT116 and MCF-7 cancer cell lines. Compounds 6o, 6m, 6d and 9b showed the highest anticancer activities against HCT116 human colon adenocarcinoma with IC50 of 7±0...
April 12, 2018: Anti-cancer Agents in Medicinal Chemistry
Tereza Cristina Costa Silva, Noelio de Jesus Menezes-Filho, Giselle Pinto de Faria Lopes, Diego Madureira de Oliveira, Ezequiel Pereira, Bruno Penas Seara Pitanga, Eudes S Velozo, Songeli Menezes Freire, Jorge Clarencio de Souza Andrade, Helena Lobo Borges, Stevens Kastrup Rehen, Vivaldo Moura-Neto, Silvia Lima Costa
A glioblastoma is a primary CNS tumor that is more aggressive and lethal than other brain tumors. Its location, rapid proliferation, invasive growth, angiogenesis and immunosuppression are the main factors that limit its treatment, making it a major challenge to neuro-oncology. OBJECTIVE: This study investigated the in vitro effects of the alkaloid dihydrochelerythrine (DHC), which is extracted from Zanthoxylum stelligerum, on the viability, proliferation, cell death and b-catenin, NFkB, STAT3/pSTAT3 and interleukins roles...
April 12, 2018: Anti-cancer Agents in Medicinal Chemistry
Raquel Ciuvalschi Maia, Michelle X G Pereira, Amanda S O Hammes, Flavia C Vasconcelos, Aline R Pozzo, Thais Hancio Pereira, Ernesto R Caffarena, Cerli R Gattass
BACKGROUND: Acute myeloid leukemia (AML) represent the largest number of annual deaths from hematologic malignancy. In the United-States, it is estimated that 21.380 individuals will be diagnosed with AML and 49.5% of patients will die in 2017. Therefore, the searching for novel compounds capable of increasing the overall survival rate to the treatment of AML cells is urgent. OBJECTIVES: To investigate the cytotoxicity effect of the natural compound PA and to explore the mechanism of action of PA in AML cell lines with different phenotypes...
April 12, 2018: Anti-cancer Agents in Medicinal Chemistry
Bahareh Movafegh, Razieh Jalal, Zobeideh Mohammadi
OBJECTIVE: Cell resistance to doxorubicin and its toxicity to healthy tissue reduce its efficiency. The use of cell penetrating peptides as drug delivery system along with doxorubicin is a strategy to reduce its side effects. In this study, the influence of poly-L-arginine on doxorubicin cytotoxicity, its cellular uptake and doxorubicin-induced apoptosis on human prostate cancer DU145 cells are assessed. METHODS: The cytotoxicity of doxorubicin and poly-L-arginine, alone and in combination, in DU145 cells was evaluated at different exposure times using MTT assay...
April 11, 2018: Anti-cancer Agents in Medicinal Chemistry
M Asad Khan, Md Zafaryab, Syed M Hassan, Irfan Ahmad, Moshahid A Rizvi
Curcumin is a potent anticancer agent and has great potential efficacy against different types of cancers. A major disadvantage of curcumin, however, is its poor solubility and bioavailability. The aim of the present work is to synthesize chitosan and curcumin-loaded chitosan nanoparticles and their characterization through various physicochemical methods and cellular uptake in cervical cancer cell line SiHa. The studies presented demonstrate that curcumin-loaded chitosan nanoparticles showed increased uptake in the SiHa cells as compared to free curcumin and chitosan nanoparticles did not show any significant uptake in SiHa cell line...
April 11, 2018: Anti-cancer Agents in Medicinal Chemistry
Xin Ren, Wen-Hua Shan, Lu-Lu Wei, Chan-Chan Gong, Dong-Sheng Pei
BACKGROUND: Tartrate-resistant acid phosphatase 5 (ACP5) is an evolutionarily conserved and multifunctional protein that is involved in generations of reactive oxygen species, normal bone development, osteoblast regulation and macrophage function, affecting a series of pathways, as well as reflecting bone resorption and osteoclast activity. METHODS: Literature searches, systematic reviews and assessments about the structure, distribution, regulation and novel functions of ACP5 were performed in this review from PubMed and Medline databases...
April 11, 2018: Anti-cancer Agents in Medicinal Chemistry
Yanan Niu, Renyikun Yuan, Hongwei Gao, Qi Kong, Jin-Jian Lu, Xiuping Chen
There are inconsistent reports about the role of nitric oxide (NO) in cancer progression and prevention. Quinones demonstrate significant anti-cancer activities both in vitro and in vivo. Here, we reported that 2-methoxy-6-acetyl-7-methyljuglone (MAM), a natural naphthoquinone isolated from Polygonum cuspidatum Sieb. et Zucc, induced inducible nitric oxide synthase (iNOS)/NO-mediated DNA damage response through activation of MAPKs pathways in BEL-7402 and A549 cells. MAM induced DNA damage by activating ATM/Chk2...
April 10, 2018: Anti-cancer Agents in Medicinal Chemistry
Francesco Perri, Franco Ionna, Giuseppina Della Vittoria Scarpati, Francesco Longo, Raffaele Addeo, Roberto Manzo, Paolo Muto, Salvatore Pisconti, Luigi Leopaldi, Francesco Caponigro
BACKGROUND: Squamous cell carcinoma of the head and neck (SCCHN) are neoplasms arising from the epithelium of the first aero-digestive tract. They are very heterogeneous both clinically and biologically. Classic and well acknowledged risk factors are alcohol and tobacco consumption and other forms of smokeless tobacco assumption, although lately the incidence of human papilloma virus (HPV)-related SCCHN is rapidly increasing. HPV-related tumors are very different from their alcohol and tobacco-associated counterpart, as they show strong chemo and radio sensitivity and thus can often be treated with conservative treatment strategies...
April 10, 2018: Anti-cancer Agents in Medicinal Chemistry
Amany Belal
For further exploration of the promising pyrrolizine scaffold and in continuation of our previous work, that proved the potential anticancer activity of the hit compound I, a new series of pyrrolizines 2-5 and 7-9 were designed and synthesized. Structures of the new compounds were confirmed by IR, 1H-NMR, 13C-NMR and elemental analysis. Antitumor activity for the prepared compounds against human breast adenocarcinoma (MCF-7), liver (HEPG2) and colon (HCT116) cancer cell lines was evaluated using SRB assay method...
April 9, 2018: Anti-cancer Agents in Medicinal Chemistry
Banu Aydin, Hulya Cabadak, Zafer Mehmet Goren
Many studies suggested that acetylcholine (ACh) might serve as an autocrine/ paracrine growth factor in several types of tumors or tumor cell lines. Therefore, cholinergic signaling seems to be functionally important in cancer. High levels of acetylcholinesterase (AChE) activity have been reported in primary brain tumors, ovarian, colon and lung tumors. K562 cells were derived from a chronic myelogenous leukemia patient during blast crisis serving as pluripotent hematopoietic stem cells. K562 cells were incubated with various cholinergic agonists or antagonists to investigate the role of ACh in different differentiated cell lines...
April 6, 2018: Anti-cancer Agents in Medicinal Chemistry
Pankaj Attri, Ji Hoon Park, Anser Ali, Eun Ha Choi
OBJECTIVE: The aim of the paper is to investigate the optimum condition for generation of plasma activated media (PAM), where it can deactivate the cancer cells while minimum damage for normal cells. BACKGROUND: Over past few years, cold atmospheric plasma-activated media (PAM) have shown its promising application in plasma medicine for treatment of cancer. PAM has a tremendous ability for selective anti-cancer capacity in vitro and in vivo. METHOD: We have analyzed the radicals in air using the optical emission spectroscopy and in culture media using chemical analysis...
April 6, 2018: Anti-cancer Agents in Medicinal Chemistry
Leili Asadi, Sakine Shirvalilou, Sepideh Khoee, Samideh Khoei
Despite the development of conventional therapies, include surgery, radiotherapy, chemotherapy and hyperthermia, the prognosis remains very poor. Recently, integration of conventional therapy and multifunctional nanoparticles have attracted a lot of attention because it produces a synergistic effect and better diagnostic and therapeutic efficiency. OBJECTIVE: This study aimed to investigate the uptake and cytotoxic effects of polycaprolactone (PCL)/chitosan (CHI)-coated superparamagnetic iron oxide nano-graphene oxide (SPION-NGO) as a carrier of 5-fluorouracil (5-Fu) and radiofrequency (RF) hyperthermia using an alternate magnetic field (AMF) with 13...
April 4, 2018: Anti-cancer Agents in Medicinal Chemistry
Tanushree Pal, Asmita Sharda, Bharat Khade, C S Ramaa, Sanjay Gupta
Cancer chemotherapy is associated with limitations like dose dependent host-tissue toxicity, multiple drug resistance and tumor heterogeneity. Hence, it is imperative to unearth novel targets to cure cancer. At present, 'pharmaco-epigenomics' constitutes the hope in cancer treatment owing to epigenetic deregulation- a reversible process, suspected of playing a role in malignancy. In this research work, we have used the fundamentals of drug repurposing for a set of our previously synthesized difluorinated propanediones and evaluated them for their histone methyltransferase inhibitory potential in leukemic cell lines...
April 4, 2018: Anti-cancer Agents in Medicinal Chemistry
Dariusz Matosiuk
Receptors of glutamic acid are known for over 30 years for their action and for about 20 years for their structure. Presence of at least three classes of ionotropic receptors was confirmed at the beginning of 80' [1]. Recognition of the sequence [2,3] and first cloning were done at the beginning of 90' [4-6]. In 1994 ligand binding site was recognized at the junction of two subunits S1-S2 in the ligand binding domain [7]. Since then many subtypes of ionotropic and metabotropic glutamate receptors were recognized, together with their localization and functions...
April 4, 2018: Anti-cancer Agents in Medicinal Chemistry
Da-You Ma, Li-Chao Zhang, Kun-Jian Peng, Jiang Zeng, Li-Jun Liu, Zhi-Yong Luo, Su-You Liu
A series of 7-O-aminoalkyl-2,3-dehydrosilibinin derivatives were synthesized and evaluated for their antiproliferative activities against several cancer cell lines. A number of them exhibited greatly enhanced potency with 50% growth inhibition at low micromolar concentrations. Structure activity study indicated that the distance between N and 7-O on the side chain has a limited influence on the antiproliferative activity, while the presence of a morpholino group decreases the antiproliferative activities dramatically...
April 2, 2018: Anti-cancer Agents in Medicinal Chemistry
Vladimir G Bespalov, Valerij A Alexandrov, Galina I Vysochina, Vera A Kostikova, Alexandr L Semenov, Denis A Baranenko
BACKGROUND: The meadowsweet (Filipendula ulmaria (L.) Maxim.) may have a cancer prophylactic activity, since its extracts exhibits antioxidant, antiinflammatory and other effects. We investigated the ability of a meadowsweet decoction to inhibit mammary carcinogenesis induced by intramammary injections of methylnitrosourea (MNU) to the target organ in rats. MATERIALS AND METHODS: The chemical composition of meadowsweet extracts was studied by traditional methods...
April 2, 2018: Anti-cancer Agents in Medicinal Chemistry
Karakaya Gulsah, Ercan Ayse, Oncu Selin, Aytemir Mutlu Dilsiz
In the present study, Mannich bases of kojic acid with the structure of 2-substituted-3-hydroxy-6-hyroxymethyl/chloromethyl/methyl/morpholinomethyl/piperidinylmethyl/pyrrolidinylmethyl-4H-pyran-4-one (compounds 1-23) were synthesized by the reaction of kojic acid/chlorokojic acid/allomaltol and substituted benzylpiperazine derivatives in presence of formaline. To obtain the cyclic amine (morpholine, piperidine and pyrrolidine) derivatives of the 6th-position of chlorokojic acid derivatives, nucleophilic substitutions were carried out...
April 2, 2018: Anti-cancer Agents in Medicinal Chemistry
Leyla Yurttas, Bahar Demir, Gulsen Akalin Ciftci
BACKGROUND: Thiazole ring is an outstanding structure found in many biologically active compounds and clinically available drugs. Because of synthesis simplicity of its derivatives and having a wide range of biological aspects along with high effectiveness, new thiazole derivatives have been studied by medicinal chemists since many years. OBJECTIVE: Therefrom some thiazole compounds combined with different heterocyclic rings were acquired in this study. Novel 5-(4-substituted benzylidene)-2-[(4,5-dimethylthiazol-2-yl)amino]thiazol-4(5H)-one derivatives (4a-g) and 2-(heteroaryl-2/3/5-yl)thio-N-(4,5-dimethylthiazol-2-yl)acetamide (4h-p) derivatives were synthesized starting from 2-amino-4,5-dimethylthiazole...
March 27, 2018: Anti-cancer Agents in Medicinal Chemistry
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