18002-44-3Relevant academic research and scientific papers
Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant
Fukuda, Tsutomu,Anzai, Mizuho,Nakahara, Akane,Yamashita, Kentaro,Matsukura, Kazuaki,Ishibashi, Fumito,Oku, Yusuke,Nishiya, Naoyuki,Uehara, Yoshimasa,Iwao, Masatomo
supporting information, (2021/02/09)
Azalamellarin N, a synthetic lactam congener of the marine natural product lamellarin N, and its A-ring-modified analogues were synthesized and evaluated as potent and non-covalent inhibitors of the drug-resistant epidermal growth factor receptor T790M/L8
SMALL MOLECULE COMPOUNDS TARGETING PBX1 TRANSCRIPTIONAL COMPLEX
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Paragraph 0141, (2016/11/14)
In accordance with one or more embodiments, the present invention provides a compound of formulas I, II, and III, for use in methods of inhibition of PBX1-DNA interaction in a mammalian cell or population of cells, and for use in the treatment of medical
Synthesis and evaluation of C-ring aromatized analogues of phenanthridone alkaloids
Lee, Seokwoo,Hwang, Soonho,Yu, Shuai,Jang, Wonyoung,Lee, Yun Mi,Kim, Sanghee
, p. 1065 - 1070 (2012/07/14)
Phenanthridone alkaloids are envisaged as an attractive lead for the development of anticancer agents. We have prepared a series of aromatized analogues on the basis of the structure of this class of alkaloids with the hope of finding the simplified compounds with comparable activities. The obtained analogues were evaluated for their cytotoxic effect against several cancer cell lines and found to be virtually inactive. These observations together with molecular modeling studies strongly suggest that the stereochemistries of hydroxyl groups in C-ring of phenanthridone alkaloids are crucial to biological effects.
SUBSTITUTED N-ARYL BENZAMIDES AND RELATED COMPOUNDS FOR TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES
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Page/Page column 87-88, (2008/06/13)
Substituted diaryl compounds of the Formulae (I, II, III), where the variables are as defined in the claims, and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided.
New non peptidic C5a receptor antagonists
Astles, Peter C.,Brown, Thomas J.,Cox, Paul,Halley, Frank,Lockey, Peter M.,McCarthy, Clive,McLay, Iain M.,Majid, Tahir N.,Morley, Andrew D.,Porter, Barry,Ratcliffe, Andrew J.,Walsh, Roger J.A.
, p. 907 - 912 (2007/10/03)
A series of phenylguanidines which bind to the C5a receptor has been developed. The lead compound 1 (IC50 = 30 μM), discovered through random screening, has been modified to provide 32 (RPR121154) with submicromolar activity. This compound was
HETEROCYCLIC HYDRAZIDE DERIVATIVES OF MONOCYCLIC BETA-LACTAM ANTIBIOTICS
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, (2008/06/13)
Antibacterial activity has been found in compounds of the formula. Compounds having the formula and pharmaceutically acceptable salts thereof, wherein: A is a bond or alkylene; Q completes a 5- or 6-membered saturated or unsaturated(including aromatic) heterocyclic ring having one or two, hetero atoms in the ring selected from nitrogen sulfur or oxygen; X is attached to an available carbon atom in the heterocyclic ring and is hydrogen or oxo; Y is attached to an available carbon atom in the heterocyclic ring and is hydrogen, amino, hydroxyl, halogen, carboxamide, nitrile, or carboxyl, except that Y is not carboxyl when the bicyclic ring completed by Q is 2-quinolyl, 3-quinolyl, or quinoxalyl; and the remaining symbols are as defined in the specification
Heteroaryl derivatives of monocyclic beta-lactam antibiotics
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, (2008/06/13)
Compounds having the formula STR1 exhibiting antibacterial activity.
Cardiovascular activity of aromatic guanidine compounds.
Hughes et al.
, p. 1077,1080 (2007/10/04)
A series of aromatic guanidines and several 1-phenylbiguanides was prepared and tested for cardiovascular (CV) effects in anesthetized dogs measuring heart rate, blood pressure, carotid artery blood flow, and myocardial force changes. The predominant CV effect at minimally effective dose was vasoconstriction unassociated with cardiac stimulation. The structure-activity relationships of the compounds were discussed comparing their structural similarities to the beta-phenylethylamines. The most potent members of the series were phenylguanidines substituted in the 3 and 4 positions on the aromatic nucleus with hydroxy or chloro groups. Preliminary mechanism studies indicated that the 3,4-dihydroxyphenylguanidines act at least partially by a direct alpha-adrenergic mechanism
