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Synthesis and characterization of cyclohexane-1R,2R-diamine-based Pt(iv) dicarboxylato anticancer prodrugs: their selective activity against human colon cancer cell lines.

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Three pairs of asymmetric dicarboxylato derivatives based on the cisplatin and oxaliplatin-like skeletons have been synthesized de novo or re-synthesized. The axial ligands consist of one medium-chain fatty acid (MCFA), namely clofibrate (i.e. 2-(p-chlorophenoxy)-2-methylpropionic acid, CA),

Anticancer activity of newly synthesized 1,1-disubstituted cyclohexane-1-carboxamides: in vitro caspases mediated apoptosis activators in human cancer cell lines and their molecular modeling.

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Novel 1,1-disubstituted cyclohexane-1-carboxamides 6a-h, 7a-e, and 8a-b were designed and synthesized as apoptotic inducers. Cytotoxicity test revealed that some compounds have strong to moderate effect, while others displayed weak action against different cancer cell lines including, MCF-7, HepG2,

TBECH, 1,2-dibromo-4-(1,2 dibromoethyl) cyclohexane, alters androgen receptor regulation in response to mutations associated with prostate cancer.

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Point mutations in the AR ligand-binding domain (LBD) can result in altered AR structures leading to changes of ligand specificity and functions. AR mutations associated to prostate cancer (PCa) have been shown to result in receptor activation by non-androgenic substances and anti-androgenic drugs.

Novel 2-step synthetic indole compound 1,1,3-tri(3-indolyl)cyclohexane inhibits cancer cell growth in lung cancer cells and xenograft models.

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BACKGROUND The clinical responses to chemotherapy in lung cancer patients are unsatisfactory. Thus, the development of more effective anticancer drugs for lung cancer is urgently needed. METHODS A 2-step novel synthetic compound, referred to as 1,1,3-tri(3-indolyl)cyclohexane (3-indole), was

Optimization of (1,2-diamino-cyclohexane)platinum(II)-loaded polymeric micelles directed to improved tumor targeting and enhanced antitumor activity.

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Polymeric micelles are promising nanocarriers, which might enhance the efficacy of antitumor drugs. Herein, polymeric micelles incorporating dichloro(1,2-diamino-cyclohexane)platinum(II) (DACHPt), the oxaliplatin parent complex, were prepared through the polymer-metal complex formation of DACHPt

Synthesis, characterization, radiolabeling and biodistribution of a novel cyclohexane dioxime derivative as a potential candidate for tumor imaging.

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OBJECTIVE Dioxime derivative is reported to exhibit high affinity towards tumor cells. The objective of the present study is to synthesize a new dioxime derivative to be labeled with technetium-99m for using as a solid tumor marker. METHODS ((2E,2',3E,3')-3,3'-(cyclohexane-1,2-diylbis

Heterocyclization of 2-(2-phenylhydrazono)cyclohexane-1,3-dione to Synthesis Thiophene, Pyrazole and Pyridazine Derivatives with Anti-Tumor and Tyrosine Kinase Inhibitions.

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Recently hexa-hydrobenzo[d]thiazole derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Through the market it was found that many pharmacological drugs containing the thiazole nucleus were

Crotepoxide, a novel cyclohexane diepoxide tumor inhibitor from Croton macrostachys.

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Tumor inhibitors. XLV. Crotepoxide, a novel cyclohexane diepoxide tumor inhibitor from Croton macrostachys.

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Taxol resistance and its reversal by synthetic isoprenoids in human bladder cancer cell line.

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OBJECTIVE We investigated the mechanism of action of reversal agents for taxol-resistance in bladder cancers. METHODS We isolated a taxol-resistant cell line (KK47/TX30) from a human KK47 bladder cancer cell line (KK47/WT). We characterized KK47/TX30 cells and screened reversal agents for

Reversal of P-glycoprotein-mediated paclitaxel resistance by new synthetic isoprenoids in human bladder cancer cell line.

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We isolated a paclitaxel-resistant cell line (KK47/TX30) from a human bladder cancer cell line (KK47/WT) in order to investigate the mechanism of and reversal agents for paclitaxel resistance. KK47/TX30 cells exhibited 700-fold resistance to paclitaxel and cross-resistance to vinca alkaloids and

A new polyoxygenated cyclohexane and other constituents from Kaempferia rotunda and their cytotoxic activity.

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The isolation of secondary metabolites from a methanolic extract of Kaempferia rotunda yielded 12 compounds (1-12), including a new polyoxygenated cyclohexane compound, (-)-3-acetyl-4-benzoyl-1-benzoyloxymethyl-1,6-diepoxycyclohexan-2,3,4,5-tetrol (1). The structures of the isolated compounds were

SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo.

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The ability of the second generation phosphodiesterase 4 inhibitor SB 207499 (Ariflo), [c-4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)-r-l-cyclohexane carboxylic acid], to inhibit inflammatory cytokine production in vivo was evaluated and compared to that of rolipram, a first generation

Improvement of sensitivity to platinum compound with siRNA knockdown of upregulated genes in platinum complex-resistant ovarian cancer cells in vitro.

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It is known that some cancers show platinum complex resistance and that others show platinum complex sensitivity among ovarian cancers. Oxaliplatin (cis-[oxalato[trans-l-1, 2-diamino-cyclohexane] platinum[II]]; l-OHP), an active anti-cancer agent consisting of platinum, inhibits RNA synthesis and

Trastuzumab-resistant breast cancer cells remain sensitive to the auger electron-emitting radiotherapeutic agent 111In-NLS-trastuzumab and are radiosensitized by methotrexate.

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Our goals in this study were to determine whether (111)In-trastuzumab coupled to peptides harboring nuclear localizing sequences (NLSs) could kill trastuzumab-resistant breast cancer cell lines through the emission of Auger electrons and whether the combination of radiosensitization with

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