Search Results - "MERLINI, Lucio"
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1
Total Synthesis of the Natural Product Benzo[j]fluoranthene-4,9-diol: An Approach to the Synthesis of Oxygenated Benzo[j]fluoranthenes
Published in Journal of organic chemistry (01-11-2013)“…A synthetic sequence to the benzo[j]fluoranthene nucleus is described. Crucial steps of the procedure include a Suzuki coupling between appropriately…”
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2
Natural and semisynthetic azaphilones as a new scaffold for Hsp90 inhibitors
Published in Bioorganic & medicinal chemistry (15-08-2010)“…A series of mold metabolites of Ascomycetes, structurally belonging to the class of azaphilones, were found to inhibit the heat shock protein Hsp90. In…”
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3
Preclinical profile of antitumor activity of a novel hydrophilic camptothecin, ST1968
Published in Molecular cancer therapeutics (01-07-2008)“…ST1968 is a novel hydrophilic camptothecin (CPT) derivative of the 7-oxyiminomethyl series. Because ST1968 retained ability to form remarkably stable cleavable…”
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4
Synthesis and Antifungal Activity of a Series of N-Substituted [2-(2,4-Dichlorophenyl)-3-(1,2,4-triazol-1-yl)]propylamines
Published in Journal of agricultural and food chemistry (03-10-2007)“…A series of N-mono- or N,N-disubstituted [2-(2,4-dichlorophenyl-3-(1,2,4-triazol-1-yl)]propylamines and…”
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5
Optimized Synthesis and Enhanced Efficacy of Novel Triplex-Forming Camptothecin Derivatives Based on Gimatecan
Published in Bioconjugate chemistry (15-04-2009)“…Sequence-specific camptothecins are useful tools to inhibit specifically gene expression. The camptothecins are attached to the 3′ end of triplex-forming…”
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6
Current status and perspectives in the development of camptothecins
Published in Current pharmaceutical design (01-01-2002)“…Camptothecins are cytotoxic agents with a wide spectrum of antitumor activity. The unique mechanism of action, the impressive preclinical efficacy and the…”
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7
Monatin, Its Stereoisomers and Derivatives: Modeling the Sweet Taste Chemoreception Mechanism
Published in European Journal of Organic Chemistry (01-06-2005)“…The sweet natural compound monatin 1 has two stereogenic centers, and the 2S,4S absolute configuration has been attributed previously to the natural isomer…”
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Pattern of Antitumor Activity of a Novel Camptothecin, ST1481, in a Large Panel of Human Tumor Xenografts
Published in Clinical cancer research (01-12-2002)“…Purpose: ST1481 is the lead compound of a novel series of 7-modified camptothecins, the 7-oxyimino methyl derivatives, characterized by potent topoisomerase I…”
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9
Structure elucidation of clavilactone D: an inhibitor of protein tyrosine kinases
Published in Phytochemistry (Oxford) (01-04-2000)“…Clavilactones D and E were isolated from an agar culture of the Basidiomycetous fungus Clitocybe clavipes, and their structure was elucidated by 1 H - and 13 C…”
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10
Synthesis of photoactivable inhibitors of osteoclast vacuolar ATPase
Published in Bioorganic & medicinal chemistry (15-05-2003)“…Amides of (2 Z,4 E)-5-[(5,6-dichloroindol-2-yl)]-2-methoxy- N-[3-[4-[3-(carboxymethoxy)phenyl)] piperazin-1-yl]propyl]-2,4-pentadienamide ( 1) and of…”
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11
A New 3,4-seco-Lupane Derivative from Lasianthus gardneri
Published in Journal of natural products (Washington, D.C.) (01-05-2004)“…A new seco-ring A lupane triterpene derivative (1), along with lupenone, lupeol, β-sitosterol, ursolic acid, and stigmasterol 3-O-β-d-glucoside, were isolated…”
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12
7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors
Published in Bioorganic & medicinal chemistry (01-02-2014)“…[Display omitted] 7-Azaindole-1-carboxamides were designed as a new class of PARP-1 inhibitors. The compounds displayed a variable pattern of target inhibition…”
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13
Abstract 3096: Host antitumor immune response activated by Dual POLA1-HDAC11 inhibitors endowed with a large spectrum of antitumor activity
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Small molecule modulators of chromatin modifying enzymes became the focus of drug discovery efforts, because of their direct antitumor effects, such…”
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14
Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D
Published in Bioorganic & medicinal chemistry (15-08-2011)“…A novel 5-oxa-6a,8-diazaindeno[2,1-b]phenanthren-7-one scaffold was designed and synthesized as an active analogue of the cytotoxic marine alkaloid Lamellarin…”
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15
Enantioselective total synthesis and absolute configuration of the alleged structure of crassinervic acid
Published in Tetrahedron (26-08-2011)“…An enantioselective synthesis of the structure reported for the natural antifungal compound, (−)-crassinervic acid ( 1), has been achieved starting from…”
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Abstract 4848: Preclinical antitumor activity of novel DNA polymerase 1 (POLA1) inhibitors
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract The anti-proliferative and pro-apoptotic effects of Retinoid-Related Molecules (RRMs) are described as independent from Retinoids' receptors-mediated…”
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Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
Published in European journal of medicinal chemistry (01-05-2009)“…A series of hydroxamic acid-based histone deacetylase (HDAC) inhibitors were designed on the basis of a model of the HDAC2 binding site and synthesized. They…”
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Abstract 4195: MIR002: a new POLA1 inhibitor endowed with a large spectrum of antitumor activity
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Abstract A recent work from Han et al. disclosed DNA polymerase 1 alpha (POLA1) as the key target for the anti-cancer effects of CD437, a molecule belonging to…”
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19
First total synthesis of topopyrone C
Published in Tetrahedron letters (05-02-2007)“…The first synthesis of topopyrone C, a natural compound and inhibitor of Topoisomerase I, has been carried out by Marschalk alkylation of…”
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20
Synthesis of (+)-Spirolaxine Methyl Ether
Published in Journal of organic chemistry (04-08-2006)“…A short and efficient synthesis of (+)-spirolaxine methyl ether, a metabolite of the fungus Sporotrichum laxum with inhibitory activity against Helicobacter…”
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