34798-68-0Relevant academic research and scientific papers
Discovery and structure-activity relationship of N-phenyl-1H-pyrazolo[3,4-b]quinolin-4-amines as a new series of potent apoptosis inducers
Zhang, Han-Zhong,Claassen, Gisela,Crogran-Grundy, Candace,Tseng, Ben,Drewe, John,Cai, Sui Xiong
, p. 222 - 231 (2008/09/16)
We report the discovery and SAR study of a series of N-phenyl-1H-pyrazolo[3,4-b]quinolin-4-amines as potent inducers of apoptosis. N-(3-Acetylphenyl)-2,3-dihydro-1H-cyclopenta[b]quinolin-9-amine (2) was discovered through our cell- and caspase-based HTS assays as an inducer of apoptosis. Compound 2 is active against cancer cells derived from several human solid tumors, with EC50 values ranging from 400 to 700 nM. SAR study of hit 2 led to the discovery of N-phenyl-1H-pyrazolo[3,4-b]quinolin-4-amines as a novel series of potent apoptosis inducers, with 1,3-dimethyl-N-(4-propionylphenyl)-1H-pyrazolo[3,4-b]quinolin-amine (6b) having EC50 values ranging from 30 to 70 nM in cancer cells. These compounds also demonstrated potent activity in the cell growth inhibition assay, with GI50 values of 16-42 nM for compound 6b.
SUBSTITUTED N-ARYL-1H-PYRAZOLO[3,4-b]QUINOLIN-4-AMINES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS
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Page/Page column 36, (2008/06/13)
The present invention is directed to substituted N-aryl-1H-pyrazolo[3,4-b]quinolin-4-amines and analogs thereof, represented by the general Formula (I): wherein Q, Y, Z, R4-R7, X and Ar are defined herein. The present invention also
Method for inhibiting neoplastic cells and related conditions by exposure to substituted N- arylmethyl and heterocyclmethyl-1H-pyrazolo (3,4-B) quinolin-4-amines
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, (2008/06/13)
A method for inhibiting neoplastic cells and related conditions by exposing them to substituted N-arylmethyl and heterocyclmethyl-1H-pyrazolo?3,4-B!quinolin-4-amines.
Substituted N-arylmethyl and heterocyclmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines and compositions and methods of use thereof
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, (2008/06/13)
Substituted N-arylmethyl and heterocyclylmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing o
An efficient solid phase synthetic route to 1,3-disubstituted 2,4(1H,3H)-quinazolinediones suitable for combinatorial synthesis
Smith, Adrian L.,Thomson, Christopher G.,Leeson, Paul D.
, p. 1483 - 1486 (2007/10/03)
Novel, efficient solid phase chemistry has been developed for the synthesis of 1,3-disubstituted quinazolinediones. Anthranilic acids are linked to a chloroformate resin through the nitrogen, amines are coupled to the flee carboxylic acid, and thermal cyclization leads to heterocycle formation and concommitant resin release resulting in traceless linkage.
