32114-73-1Relevant academic research and scientific papers
AZAQUINAZOLINE CARBOXAMIDE DERIVATIVES
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, (2014/06/23)
Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
Water-induced fluorescence quenching of mono- and dicyanoanilines
Oshima, Juro,Yoshihara, Toshitada,Tobita, Seiji
, p. 306 - 311 (2008/02/13)
Photophysical properties of monocyano- (2-, 3-, and 4-cyano) and dicyano- (3,4-, 3,5-, 2,3-, 2,4-, 2,5-, and 2,6-dicyano) anilines are investigated by fluorescence measurements. All the monocyanoanilines are virtually nonfluorescent in water (quantum yield 0.01); however, in nonaqueous solvents (cyclohexane, acetonitrile and ethanol), the fluorescence quantum yield is enhanced substantially. In contrast, dicyanoanilines investigated are highly fluorescent both in aqueous and nonaqueous environments. The photophysical data and MO calculations suggest that conformational changes in the amino group and variation of hydrogen-bonding interactions between the solute and solvent water upon electronic excitation are responsible for the water quenching in the monocyanoanilines.
Method of treating a patient having precancerous lesions with phenyl quinazolinone derivatives
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, (2008/06/13)
Derivatives of 2-phenyl quinazolinones are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit growth of neoplastic cells.
QUINAZOLINONE ANTIANGINAL AGENTS
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, (2008/06/13)
Compounds of formula: and pharmaceutically acceptable salts thereofwhereinR1 is H, Q - Q alkyl, C j -Q alkoxy or CONRsRs;R2 is H or- CJ-C4 alkyl;R3 is C2-C4 alkyl;R4 is H, C2-C4 alkanoyl optionally substituted withNR7R8, (hydroxy)C2-C4 alkyl optionally substitutedwith NR7R8, CH=CHC02R9, CH=CHCONR7R8,CH2CH2C02R9, CH2CH2CONR7R8, S02NR7R8,S02NH(CH2)nNR7R8 or imidazolyl;R5 and Rs are each independently H or C1-C4 alkyl;R7 and R8 are each independently H or C1-C4 alkyl, ortogether with the nitrogen atom to which they areattached form a pyrrolidino, piperidino, morpholino or4-(NR10)-l-piperazinyl group wherein any of saidgroups is optionally substituted with CONR5R6;R9 is H or C1-C4 alkyl;R10 is H, C1-C3 alkyl or (hydroxy)C2-C3 alkyl; andn is 2, 3 or 4;with the proviso that R4 is not H when R1 is H, C1-C4 alkylor C1-C4 alkoxy; are selective cGMP PDE inhibitors usefiilin the treatment of cardiovascular disorders such as angina, hypertension, heart failure and atherosclerosis.
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide
Clark,Deans,Stevens,Tisdale,Wheelhouse,Denny,Hartley
, p. 1493 - 1504 (2007/10/02)
A series of new imidazo[5,1-d]-1,2,3,5-tetrazinones with additional hydrogen-bonding or ionic substituents at the 8-carboxamide position of the antitumor drugs temozolomide (1) and mitozolomide (2) has been prepared. None of these compounds were significantly more cytotoxic in vitro against the mouse TLX5 lymphoma than the lead structures. Molecular modeling techniques have been used to design benzo- and pyrazolo[4,3-d]-1,2,3-triazinones bearing carboxamide groups in appropriate positions which are isosteric with temozolomide and mitozolomide but which cannot ring open to alkylating species. As predicted, these compounds have no inhibitory properties against human GM892A or Raji cell lines in vitro. Temozolomide and the spermidine- temozolomide conjugate 28 preferentially methylate guanines within guanine- rich sequences in DNA, but no experimental evidence has been found to support the hypothesis that such regions are involved in catalyzing the ring opening of the imidazotetrazinone prodrugs to their active forms.
