- Naphthyl urea compound, and preparation method and application thereof
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The invention provides a naphthyl urea compound, and a preparation method and application thereof. A naphthyl urea parent nucleus group with biological activity contained in the naphthyl urea compound is further chemically modified to generate a plurality of compounds with higher biological activity, so that the wide application of the compounds in biological medicines and the development prospect of pharmaceutical preparations are expanded. The compound can obviously inhibit proliferation of cells of liver cancer, breast cancer, lung cancer, drug-resistant lung cancer, leukemia and the like at low dosage (submicromole), induce arrest of a cell cycle G2/M phase and promote cell apoptosis, so that the compound has a prospect of being developed into an anti-tumor drug.
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Paragraph 0047; 0103-0108
(2021/06/21)
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- Naphthalene-based urea compound with brand-new chemical structure and preparation method and application thereof
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The invention discloses a naphthyl urea compound with a brand-new chemical structure and a preparation method and application thereof, wherein the naphthourea compound with the bioactive naphthalene urea mother nucleus group is further subjected to further chemical modification to generate a plurality of compound groups with higher biological activity. andSuch compounds can significantly inhibit the activation of JAK2/STAT3 signals at low doses (sub-micromoles) MTT. The compound can inhibit JAK2 signal activation and expression of downstream STAT3, CyclinD1, CyclinB1 and MMP9 and other target genes, induce cell cycle arrest and apoptosis, and obviously inhibit the proliferation of various tumor cell strains such as breast cancer, liver cancer, lung cancer, drug resistance and a prospect of targeting anti-cancer drugs JAKAKAKAKAKs/STAT3.
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Paragraph 0047; 0085-0088
(2021/09/29)
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- A novel [...] compound of preparation and its use in cancer therapy (by machine translation)
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The invention belongs to the field of biology, discloses a new naphthol compound of the design and its preparation method, and this compound or its biological acceptable salt as active ingredient preparation in cell growth control mechanism and application in cancer therapy. Through the biological activity tests show that, the invention relates to the compounds of tumor cells STAT3 cell signal transduction has obvious inhibition effect, and to lung cancer, breast cancer, colon cancer and leukemia such as the proliferation of the cancer cell is obviously antagonistic effect. This class of compounds for the treatment of cancer and cancer clinical potential mechanism to study the significance, with great potential for development, it has very good application prospect. (by machine translation)
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Paragraph 0071; 0082-0085
(2019/02/21)
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- Preparation of novel compound and application of novel compound in cancer therapy
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The invention belongs to the field of biomedicine, and provides a method of designing and preparing a novel compound, and application of the novel compound in cell growth regulatory mechanisms and cancer treatment. The bioactivity test indicates that the
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Paragraph 0040; 0043-0045
(2019/03/08)
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- A novel salicylic acid derivatives preparation method and its application in treating the tumor
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The invention belongs to the field of biological medicine, and particularly provides a novel salicylic acid derivatives and application in treating the tumor. We use the chemical synthetic method has been a series of novel salicylic acid derivatives of the compound. We found that the biological activity of the compounds to identify breast cancer, lung cancer, leukemia and other various cell strain has obvious antagonistic effect, we study found that anti-tumor mechanism of the class of compounds STAT3 cell signal transduction have prominent inhibit function, the display of these compounds for the treatment of STAT3 signal conduction abnormality types of cancer has a great significance.
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Paragraph 0018; 0030-0035
(2019/04/10)
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- Preparation method of novel benzanilide compounds and application of novel benzanilide compounds to tumor treatment
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The invention belongs to the field of biomedicine, and particularly provides a preparation method of novel benzanilide compounds and application of the novel benzanilide compounds to tumor treatment.A series of novel benzanilide compounds are obtained by using a chemical synthesis method. Biological activity identification shows that the compounds have obvious antagonistic effects on growth and reproduction of various cell strains such as breast cancer and lung cancer; research on anti-tumor mechanisms proves that the compounds have a remarkable inhibition effect on STAT3 cell signal conduction and show that the compounds have potential important significance in treating STAT3 signal conduction abnormal diseases.
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Paragraph 0030; 0035
(2019/08/12)
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- 3,5-Bis(benzylidene)-4-piperidones and related N-acyl analogs: A novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum
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Drug resistance is a major challenge in antimalarial chemotherapy. In addition, a complete cure of malaria requires intervention at various stages in the development of the parasite within the host. There are only a few antimalarials that target the liver stage of the Plasmodium species which is an essential part of the life cycle of the malarial parasite. We report a series of antimalarial 3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs 1-5, a number of which exhibit potent in vitro growth-inhibiting properties towards drug-sensitive D6 and drug-resistant C235 strains of Plasmodium falciparum as well as inhibiting the liver stage development of the malarial life cycle. The compounds 2b (IC50: 165 ng/mL), 3b (IC50: 186 ng/mL), 5c (IC50: 159 ng/mL) and 5d (IC50: 93.5 ng/mL) emerged as lead molecules that inhibit liver stage Plasmodium berghei and are significantly more potent than chloroquine (IC50: >2000 ng/mL) and mefloquine (IC50: >2000 ng/mL) in this screen. All the compounds that showed potent inhibitory activity against the P. berghei liver stage were nontoxic to human HepG2 liver cells (IC50: >2000 ng/mL). The compounds 5a and 5b exhibit comparable metabolic stability as chloroquine and mefloquine in human plasma and the most potent compound 5d demonstrated suitable permeability characteristics using the MDCK monolayer. These results emphasize the value of 3,5-bis(benzylidene)-4-piperidones as novel antimalarials for further drug development.
- Das, Umashankar,Singh, Ravi S.P.,Alcorn, Jane,Hickman, Mark R.,Sciotti, Richard J.,Leed, Susan E.,Lee, Patricia J.,Roncal, Norma,Dimmock, Jonathan R.
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p. 7250 - 7256
(2013/11/19)
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- Design, synthesis and cytotoxic properties of novel 1-[4-(2-alkylaminoethoxy)phenylcarbonyl]-3,5-bis(arylidene)-4-piperidones and related compounds
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The 3,5-bis(arylidene)-4-piperidones 1 contain the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore which is considered to interact at a complementary binding site in susceptible neoplasms. The hypothesis was formulated that the presence of an acyl group attached to the piperidyl nitrogen atom in series 1 may interact with an additional binding site thereby enhancing cytotoxic potencies. This concept led to the synthesis of various N-acyl-3,5-bis(arylidene)-4-piperidones 3-7 many of which displayed significant cytotoxicity towards a variety of cancer cell lines. A comparison of the potencies between the compounds in series 1 and the related nonquaternary analogues 3-6 revealed that in approximately half of the comparisons made, the N-acyl analogues had increased potencies.
- Das, Umashankar,Alcorn, Jane,Shrivastav, Anuraag,Sharma, Rajendra K.,De Clercq, Erik,Balzarini, Jan,Dimmock, Jonathan R.
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- Process for preparing benzoic acids
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An improved process for the preparation of 4[(2-piperidin-1-yl)ethoxy]benzoic acid derivatives, comprising reacting a haloalkyl amine of formula (III) with a compound of formula (IV) in the presence of a hydrated inorganic base in an appropriate solvent.
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Page/Page column 4-7
(2010/02/12)
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- DEVELOPMENT OF NEW SELECTIVE ESTROGEN RECEPTOR MODULATORS
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The present disclosure concerns a new class of selective estrogen receptor modulators (SERMs). The disclosure also includes the identification of a previously unknown membrane associated estrogen receptor. Methods for making and using the disclosed SERMs
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Page/Page column 33-34
(2010/02/11)
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- Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
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Novel processes for producing compounds of formula I STR1 wherein R1 and R2 each are independently C1 -C4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; and n is 2 or 3; or a pharmaceutically acceptable salt thereof employing alkylacetate solvents are provided.
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- Antiestrogens. 2. Structure-Activity Studies in a Series of 3-Aroyl-2-arylbenzothiophene Derivatives Leading to thien-3-yl>phenyl>methanone Hydrochloride (LY156758), a Remarkably Effective Estrogen Antagonist with On...
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In an effort to prepare nonsteroidal antiestrogens demonstrating greater antagonism and less intrinsic estrogenicity than those currently available, a series of 3-aroyl-2-arylbenzothiophene derivatives was synthesized.These compounds were prepared by Friedel-Crafts aroylation of appropriate O-protected 2-arylbenzothiophene nuclei with basic side-chain-bearing benzoyl chlorides followed by removal of the protective groups to provide the desired compounds containing both hydroxyl and basic side-chain functionality.A particularly useful method for the cleavage of aryl methoxy ethers without removal of (dialkylamino)ethoxy side chain functionality elsewhere in the molecule was found to be AlCl3/EtSH.The benzothiophene derivatives were tested for their ability to inhibit the growth-stimulating action of estradiol on the immature rat uterus.Seemingly minor changes in the side-chain amine moiety were found to have profound effects on the ability of the compounds to antagonize estradiol.Analogues having basic side chains containing cyclic (pyrrolidine, piperidine, and hexamethyleneamine) moieties were found to have less intrinsic estrogenicity and to antagonize estradiol action more completely than their noncyclic counterparts.The most effective antiestrogen in the series, compound 44, thien-3-yl>phenyl>methanone, elicited a modest uterotropic activity that did not increase with increasing dose.In antagonism of estradiol, 44 exhibited a degree of inhibition surpassing that of tamoxifen at any dose tested.The new benzothiophene antiestrogen was also shown to have high affinity for rat uterine cycloplasmic estrogen receptor and to be an inhibitor of the growth of DMBA-induced rat mammary tumors.
- Jones, Charles D.,Jevnikar, Mary G.,Pike, Andrew J.,Peters, Mary K.,Black, Larry J.,at al.
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p. 1057 - 1066
(2007/10/02)
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