- Synthesis and Anticancer Activity of Thiophene-2-carboxamide Derivatives and In Silico Docking Studies
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A novel series of thiophene-2-carboxamide derivatives are designed and synthesized, and their structures are confirmed by 1H and 13C NMR, and mass spectra. The synthesized compounds are evaluated for their in vitro cytotoxic activity by MTT assay. Among the tested compounds, the derivative with 4-Cl-phenyl ring exhibits potent inhibitory activity against MCF-7, K562, HepG2, and MDA-MB-231. The molecular docking study performed for the synthesized compounds against PTP1B exhibits essential key interactions.
- Gulipalli,Ravula,Bodige,Endoori,Cherukumalli,Narendra Sharath Chandra,Seelam
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- 3-Alkoxy-4-bromothiophenes: General synthesis of monomers and regio-selective preparation of two dimers
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3-Alkoxy-4-bromothiophenes were synthesized in three steps from the readily available methyl 2-carboxylate-3-hydroxythiophene and two isomers of bithiophenes based on the 3-bromo-4-methoxythiophene moiety were regio-selectively prepared.
- Savitha, Gurunathan,Hergué, Noémie,Guilmet, Erwan,Allain, Magali,Frère, Pierre
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- Design, synthesis, in silico and in vitro evaluation of thiophene derivatives: A potent tyrosine phosphatase 1B inhibitor and anticancer activity
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A series of novel methyl 4-(4-amidoaryl)-3-methoxythiophene-2-carboxylate derivatives were designed against the active site of protein tyrosine phosphatise 1B (PTP1B) enzyme using MOE.2008.10. These molecules are also subjected for in silico toxicity prediction studies and considering their corresponding drug scores, it implied that, the molecules are promising as anticancer agents. The designed compounds were synthesized by using suitable methods and characterized. They were subjected to inhibitory activity against PTP1B and in vitro anticancer activity by MTT assay. Most of the tested compounds showed potent inhibitory activity against PTP1B, among the compounds tested, compound 5b exhibited the highest activity (IC50?=?5.25?μM) and remarkable cytotoxic activity at 0.09?μM of IC50 against the MCF-7 cell line. In addition to this, compound 5c also showed potential anticancer activity at 2.22?μM of IC50 against MCF-7 and 0.72?μM against HepG2 cell lines as well as PTP1B inhibitory activity at IC50 of 6.37?μM.
- Gulipalli, Kali Charan,Bodige, Srinu,Ravula, Parameshwar,Endoori, Srinivas,Vanaja,Suresh Babu,Narendra Sharath Chandra,Seelam, Nareshvarma
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- Synthesis and Anticancer Activity of Novel Urea and Thiourea Bearing Thiophene-2-carboxalate Derivatives
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Abstract: A new series of urea and thiourea bearing thiophene-2-carboxalate derivatives has been designed against protein tyrosine phosphatase 1B (PTP1B) active site, synthesized and charecterized by 1H and 13C NMR, and mass spectra. The compounds have been evaluated for in vitro anticancer activity against different cancer cell lines using the MTT colorimetric assay and doxorubicin as a standard drug. Among the tested compounds, methyl 3-methoxy-4-{4-[3-(4-methoxyphenyl)thioureido]phenyl}thiophene-2-carboxylate demonstrates the highest inhibitory activity against MCF-7, K562, HepG2, MDA-MB-231, and HeLa cell lines. The new molecular structures and their interactions with PNP1B have been evaluated by docking studies.
- Bodige, S.,Chandra, J. N. Narendra Sharath,Cherukumalli, P. Koteswara Rao,Endoori, S.,Gulipalli, K. Ch.,Ravula, P.,Seelam, N.
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- Opioid receptor agonists and application thereof
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The invention discloses compounds and salts thereof that can be used as opioid receptor ligands, a preparation method of the compounds, compositions containing the compounds, and a use of the compounds as [mu] opioid receptor agonists; the compounds are used for treatment of [mu] opioid receptor-mediated related diseases, such as pains and pain-related disorders.
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- Synthesis of functionalized hydroxy-thiophene motifs as amido- and sulfonamido-phenol bioisosteres
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Novel highly substituted hydroxy thiophene motifs were designed and synthesized as viable amido phenol and sulfonamido phenol bioisosteres. Hydroxy group-directed regioselective bromination and palladium-catalyzed amination of thienyl bromide via Buckwald
- Chao, Jianhua,Taveras, Arthur G.,Aki, Cynthia J.
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scheme or table
p. 5005 - 5008
(2009/12/01)
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- INHIBITORS OF Akt ACTIVITY
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Invented are novel thiophene compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 178
(2010/11/27)
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- THIADIAZOLES AS CXC- AND CC- CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of Formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of Formula (IA).
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Page/Page column 157
(2010/02/12)
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- ISOTHIAZOLE DIOXIDES AS CXC- AND CC- CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of the formula (IA): and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
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Page/Page column 160; 338-339
(2010/02/13)
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- CXCR1 AND CXCR2 CHEMOKINE ANTAGONISTS
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The present invention is directed to a compound having the general structure of formula (1) useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.
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Page/Page column 77
(2010/02/14)
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- THIADIAZOLEDIOXIDES AND THIADIAZOLEOXIDES AS CXC- AND CC-CHEMOKINE RECEPTOR LIGANDS
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Disclosed are novel compounds of the formula (IA) and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula (IA).
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
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There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- 1,2,4-TRIAMINOBENZENE DERIVATIVES USEFUL FOR TREATING DISORDERS OF THE CENTRAL NERVOUS SYSTEM
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The present invention concerns 1,2,4-triaminobenzene derivatives of the general formula I or pharmaceutically acceptable salts thereof and the use thereof.
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- 3, 4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor antagonists
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Disclosed are compounds of the formula: or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are the use of compounds of formula I for the treatment of chemokine-mediated diseases such as cancer, and acute and chronic inflammatory disorders.
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- 3,4-Di-substituted cyclobutene-1,2-diones as CXC chemokine receptor antagonists
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There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or isomer of said compound or of said prodrug, which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.
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- N-([1,2,4] triazoloazinyl) thiophenesulfonamide compounds and their use as herbicides
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N-(Triazoloazinyl)thiophenesulfonamide compounds were prepared from appropriately substituted 2-amino[1,2,4]triazolo[1,5-c]pyrimidine, 2-amino[1,2,4]triazolo[1,5-a]pyrimidine and 2-amino[1,2,4]triazolo[1,5-a]pyridine compounds and appropriately substituted thiophenesulfonyl chloride compounds. The compounds were found to be useful as herbicides.
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