138764-20-2Relevant academic research and scientific papers
Seco-B-ring steroidal dienynes with aromatic D ring: Design, synthesis and biological evaluation
Szybinski, Marcin,Brzeminski, Pawel,Fabisiak, Adrian,Berkowska, Klaudia,Marcinkowska, Ewa,Sicinski, Rafal R.
, (2017)
Continuing our structure-activity studies on the vitamin D analogs with the altered intercyclic seco-B-ring fragment, we designed compounds possessing dienyne system conjugated with the benzene D ring. Analysis of the literature data and the docking exper
4H-THIENO[3,2-C]CHROMENE-BASED INHIBITORS OF NOTUM PECTINACETYLESTERASE AND METHODS OF THEIR USE
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Page/Page column 17, (2012/12/13)
Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS
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Page/Page column 54-55, (2011/06/16)
Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
Benzo[A] [phenazin-11-carboxamide derivatives and their use as joint inhibitors of topomerase I and II
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, (2008/06/13)
A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2(R11), SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR10 and N(R12)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not, to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R1 and R9, which are the same or different, are each hydrogen or C1-C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; or a pharmaceutically acceptable salt thereof; with the proviso that at least one R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.
Novel angular benzophenazines: Dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents
Vicker, Nigel,Burgess, Luke,Chuckowree, Irina S.,Dodd, Rory,Folkes, Adrian J.,Hardick, David J.,Hancox, Timothy C.,Miller, Warren,Milton, John,Sohal, Sukhjit,Wang, Shouming,Wren, Stephen P.,Charlton, Peter A.,Dangerfield, Wendy,Liddle, Chris,Mistry, Prakash,Stewart, Alistair J.,Denny, William A.
, p. 721 - 739 (2007/10/03)
A series of substituted angular benzophenazines were prepared using a new synthetic route via a novel regiocontrolled condensation of 1,2-naphthoquinones and 2,3-diaminobenzoic acids. The synthesis and biological activity of this new series of substituted
Imidazole derivatives, their preparation and their use as S-adenosylmethionine decarboxylase (=SAMDC) inhibitors
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, (2008/06/13)
Described are compounds of formula I STR1 wherein R1 is hydrogen or hydroxy; R2, R2 ' and R2 " are each independently of the others hydrogen or a substituent other than hydrogen; either R3 is hydrogen or a substituent other than hydrogen and R4 is hydrogen or lower alkyl, or R3 and R4 together form a divalent radical of the formula --(CH2)n -- wherein n is 2 or 3; R5 and R6 are each independently of the other hydrogen, alkyl or aryl; and either R7 and R8 are each hydrogen, or R7 and R8 together form a bond; tautomers thereof, provided that at least one tautomerisable group is present; and salts thereof. The compounds inhibit the enzyme S-adenosylmethionine decarboxylase and are suitable, for example, for the treatment of tumours and protozoal infections.
Aminodienylesters. I: The cycloaddition reactions of tert- aminodienylester with α,β-unsaturated carbonyl compounds, styrenes, and quinones
Koike, Takeshi,Tanabe, Mituharu,Takeuchi, Naoki,Tobinaga, Seisho
, p. 243 - 248 (2007/10/03)
Methyl 5-(N,N-dimethylamino)-2,4-pentadienoate (tert-aminodienylester 1) was synthesized by condensation of methyl crotonate (2) with N,N,N',N'- tetramethylenediamine (3). The reactivity of 1 was investigated with methyl propiolate (4), dimethyl 2-butynedionate (5), dimethyl maleate (6), dimethyl fumarate (7), 2-buten-4-olide (8), 2-cyclohexenone (9), styrene (10), trans- β-nitrostyrene (11), 1,4-benzoquinone (19), methyl 1,4-naphthoquinone-5- carboxylate (21), 1,4-naphthoquinone (24), juglone (26), 5-methoxy-1,4- naphthoquinone (28), naphthazarin (31), and naphthazarin dimethyl ether (33). In addition, 5-(N,N-dimethylamino)-2,4-pentadienenitrile (tert-aminodienyl- nitrile 37) was synthesized by condensation of crotononitrile (36) with 3. The reactivity of 37 was investigated with dimethyl 2-butynedionate (5), and 2-cyclohexenone (9).
