111511-90-1Relevant articles and documents
Water-soluble third generation antitumor platinum complexes, [2,2-bis(aminomethyl)-1,3-propanediol-N,N'][1,1-cyclobutanedicarboxylato(2- )-O,O']platinum(II) and [1,1-cyclobutanedicarboxylato(2-)-O,O'][tetrahydro-4H-pyran-4,4- dimethanamine-N,N']platinum(II)
Bitha,Carvajal,Citarella,Child,Delos Santos,Dunne,Durr,Hlavka,Lang Jr.,Lindsay,Morton,Thomas,Wallace,Lin,Haltiwanger,Pierpont
, p. 2015 - 2020 (1989)
The synthesis, stability, and antitumor activity of a series of water-soluble third generation platinum(II) complexes have been described. Among these complexes, [2,2-bis(aminomethyl)-1,3-propanediol-N,N'][1,1-cyclobutanedicarboxylato(2- )-O,O']platinum(II) and [1,1-cyclobutanedicarboxylato(2-)-O,O'](tetrahydro-4H-pyran-4,4- dimethanamine-N,N')platinum(II) have shown the greatest promise for further investigation and are currently under clinical evaluation.
Structure-activity relationship study of pyrimido[1,2-c][1,3]benzothiazin- 6-imine derivatives for potent anti-HIV agents
Mizuhara, Tsukasa,Oishi, Shinya,Ohno, Hiroaki,Fujii, Nobutaka,Shimura, Kazuya,Matsuoka, Masao
supporting information, p. 6434 - 6441,8 (2012/12/12)
3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) is an antiretroviral agent with submicromolar inhibitory activity against human immunodeficiency virus-1 (HIV-1) and HIV-2 infection. In the current study, the structure-activity relationships of accessory groups at the 3- and 9-positions of pyrimido[1,2-c][1,3]benzothiazin-6-imine were investigated for the development of more potent anti-HIV agents. Several different derivatives containing a 9-aryl group were designed and synthesized using Suzuki-Miyaura cross-coupling and Ullmann coupling reactions. Modification of the m-methoxyphenyl or benzo[d][1,3]dioxol-5-yl group resulted in improved anti-HIV activity. In addition, the 2,4-diazaspiro[5.5]undec-2-ene-fused benzo[e][1,3]thiazine derivatives were designed and tested for their anti-HIV activities. The most potent 9-(benzo[d][1,3]dioxol-5-yl) derivative was two-threefold more effective against several strains of HIV-1 and HIV-2 than the parent compound, PD 404182.
3-(AMINOARYL)-PYRIDINE COMPOUNDS
-
Page/Page column 88, (2012/06/01)
The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.
