57861-03-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors
Ji, Dezhong,Xu, Yungen,Zhang, Jing-Jing,Zhang, Wanwan
, (2020)
A series of anthranilamide derivatives were designed and synthesized as novel smoothened (SMO) inhibitors based on the SMO inhibitor taladegib (LY2940680), which can also inhibit the SMO-D473H mutant, via a ring-opening strategy. The phthalazine core in LY2940680 was replaced with anthranilamide, which retained the inhibitory activity towards the hedgehog (Hh) signaling pathway as evidenced by a dual luciferase reporter gene assay. Compound 12a displayed the best inhibitory activity against the Hh signaling pathway with IC50 value of 34.09 nM, and exhibited better proliferation inhibitory activity towards the Daoy cell line (IC50 = 0.48 μM) than LY2940680 (IC50 = 0.79 μM).
SMO (smoothened) inhibitor containing benzoylpiperidine structure and preparation and application methods thereof
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Paragraph 0072; 0074; 0075; 0076, (2019/05/22)
The invention discloses a benzoylpiperidine derivative and preparation and application methods thereof. The benzoylpiperidine derivative is a compound containing N-methyl-N-(1-(2-aminobenzoyl)piperidine-4-yl)amide structure shown as the formula I. The invention also discloses a preparation method of the benzoylpiperidine derivative. The invention also discloses application of the benzoylpiperidinederivative to preparing SMO protein inhibitors as well as application of drug combinations containing the benzoylpiperidine derivative to preparing anti-tumor drugs.
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 41, (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
